Browse result page of ThPDB2
This is the result page of the browse module of ThPDB2. This page gives the information about the query submitted by the user as per the browse category. Further details of the entries can be seen by clicking on the ID or THPP_ID. Further the user can sort the entries on the basis of various fields by clicking on the respective headers. The user can also download the results in various formats.
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| ID | THPP_ID | Therapeutic Name | Sequence | Molecular Weight | Chemical Formula | Isoelectric Point | Hydrophobicity | Melting Point | Half Life | Description | Disease/Indication | Pharmacodynamics | Mechanism of Action | Toxicity | Metabolism | Absorption | Volume of Distribution | Clearance | Categories | Patent Number | Date of Issue | Date of Expiry | Drug Interaction | Target | Brand Name | Company | Brand Description | Prescribed for | Chemical Name | Formulation | Physical Appearance | Route of Administation | Recommended Dosage | Contraindication | Side Effects | Useful Links 1 | Useful Links 2 | Remarks |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 10001 | Th1001 | Lepirudin | >Th1001_Lepirudin LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ | 6979 | C287H440N80O111S6 | 3.7 | -0.777 | 65 | Approximately 1.3 hours | Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. | For the treatment of heparin-induced thrombocytopenia. | Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches. | Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade. | In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased. | Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, conclusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) | Bioavailability is 100% following injection. | 12.2 L [Healthy young subjects (n = 18, age 18-60 years)] | 164 ml/min [Healthy 18-60 yrs] | Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombin Proteins, Antithrombins, Blood and Blood Forming Organs, Cardiovascular Agents, Enzyme Inhibitors, Fibrin Modulating Agents, Hematologic Agents, Peptides, Protease Inhibitors, Proteins, Serine Protease Inhibitors, Serpins, Thrombin Inhibitors | CA1339104 | 29-Jul-1997 | 29-Jul-2014 | Ginkgo biloba = may increase bleed risk. | Prothrombin | Refludan | Berlex Labs | Berlex Labs | heparin-induced thrombocytopenia (HIT) and associated thromboembolic disease | [Leu1, Thr2]-63-desulfohirudin | Each vial of REFLUDAN contains 50 mg lepirudin. Other ingre-dients are 40 mg mannitol and sodium hydroxide for adjust-ment of pH to approximately 7 | Sterile, white, freeze-dried powder | Intravenous infusion | Recommended dose is 0.4 mg/kg body weight (up to 110kg) slowly intravenously (eg, over 15 to 20seconds) as a bolus dose, and can be followed by 0.15 mg/kg body weight (up to 110kg)/hour as a continuous Intravenous infusion for 2 to 10 days or longer if CL. | Hypersensitivity | NA | Link | NA | NA |
| 10002 | Th1001 | Lepirudin | >Th1001_Lepirudin LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ | 6979 | C287H440N80O111S6 | 3.7 | -0.777 | 65 | Approximately 1.3 hours | Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. | For the treatment of heparin-induced thrombocytopenia. | Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches. | Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade. | In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased. | Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, conclusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) | Bioavailability is 100% following injection. | 18.7 L [Healthy elderly subjects (n = 10, age 65-80 years)] | 139 ml/min [Healthy 65-80 yrs] | Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombin Proteins, Antithrombins, Blood and Blood Forming Organs, Cardiovascular Agents, Enzyme Inhibitors, Fibrin Modulating Agents, Hematologic Agents, Peptides, Protease Inhibitors, Proteins, Serine Protease Inhibitors, Serpins, Thrombin Inhibitors | US5180668 | 19-Jan-1993 | 6-Mar-2012 | Treprostinil = increases the risk of bleeding when combined with Lepirudin. | NA | NA | Bayer Healthcare | Bayer Healthcare | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 10003 | Th1001 | Lepirudin | >Th1001_Lepirudin LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ | 6979 | C287H440N80O111S6 | 3.7 | -0.777 | 65 | Approximately 1.3 hours | Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. | For the treatment of heparin-induced thrombocytopenia. | Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches. | Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade. | In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased. | Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, conclusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) | Bioavailability is 100% following injection. | 18 L [Renally impaired patients (n = 16, creatinine clearance below 80 mL/min)] | 61 ml/min [renal impaired] | Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombin Proteins, Antithrombins, Blood and Blood Forming Organs, Cardiovascular Agents, Enzyme Inhibitors, Fibrin Modulating Agents, Hematologic Agents, Peptides, Protease Inhibitors, Proteins, Serine Protease Inhibitors, Serpins, Thrombin Inhibitors | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 10004 | Th1001 | Lepirudin | >Th1001_Lepirudin LTYTDCTESGQNLCLCEGSNVCGQGNKCILGSDGEKNQCVTGEGTPKPQSHNDGDFEEIPEEYLQ | 6979 | C287H440N80O111S6 | 3.7 | -0.777 | 65 | Approximately 1.3 hours | Lepirudin is identical to natural hirudin except for substitution of leucine for isoleucine at the N-terminal end of the molecule and the absence of a sulfate group on the tyrosine at position 63. It is produced via yeast cells. | For the treatment of heparin-induced thrombocytopenia. | Lepirudin is used to break up clots and to reduce thrombocytopenia. It binds to thrombin and prevents thrombus or clot formation. It is a highly potent, selective, and essentially irreversible inhibitor of thrombin and clot-bond thrombin. Lepirudin requires no cofactor for its anticoagulant action. Lepirudin is a recombinant form of hirudin, an endogenous anticoagulant found in medicinal leeches. | Lepirudin forms a stable non-covalent complex with alpha-thrombin, thereby abolishing its ability to cleave fibrinogen and initiate the clotting cascade. The inhibition of thrombin prevents the blood clotting cascade. | In case of overdose (eg, suggested by excessively high aPTT values) the risk of bleeding is increased. | Lepirudin is thought to be metabolized by release of amino acids via catabolic hydrolysis of the parent drug. However, conclusive data are not available. About 48% of the administration dose is excreted in the urine which consists of unchanged drug (35%) | Bioavailability is 100% following injection. | 32.1 L [HIT patients (n = 73)] | 114 ml/min [HIT (Heparin-induced thrombocytopenia)] | Amino Acids, Peptides, and Proteins, Anticoagulants, Antithrombin Proteins, Antithrombins, Blood and Blood Forming Organs, Cardiovascular Agents, Enzyme Inhibitors, Fibrin Modulating Agents, Hematologic Agents, Peptides, Protease Inhibitors, Proteins, Serine Protease Inhibitors, Serpins, Thrombin Inhibitors | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10145 | Th1021 | Thyrotropin Alfa | >Th1021_Thyrotropin_Alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 | 25 ± 10 hours | Thyrotropin alfa is a recombinant form of thyroid stimulating hormone used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients. | For detection of residueal or recurrent thyroid cancer | Binding of thyrotropin alfa to TSH receptors on normal thyroid epithelial cells or on well-differentiated thyroid cancer tissue stimulates iodine uptake and organification. Thyrogen is an exogenous source of human TSH that offers an additional diagnostic tool in the follow-up of patients with a history of well-differentiated thyroid cancer. | Binding of thyrotropin Alfa to the thyrotropin receptors found on any residual thyroid cells or tissues stimulates radioactive iodine uptake for better radiodiagnostic imaging. | NA | NA | Time to peak: Median: 10 hours (range: 3-24 hours) After a single intramuscular injection of 0.9 mg of thyrotropin alfa: Cmax= 116+38mU/L, Tmax=22+8.5 hours. AUC=5088+1728 mU·hr/L. | NA | Through kidney and liver | Agents used to treat hypothyroidism, Anterior Pituitary Lobe Hormones and Analogues, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Pituitary and Hypothalamic Hormones and Analogues, Pituitary Hormones, Pituitary Hormones, Anterior, Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins, Thyroid Products | US5840566 | 24-Nov-1998 | 24-Nov-2015 | NA | Thyrotropin receptor | Thyrogen | Genzyme Corporation , Genzyme Europe Bv | Genzyme Corporation , Genzyme Europe Bv | It is used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients who have had their thyroid gland removed because of thyroid canc | NA | Each vial of THYROGEN contains 1.1 mg thyrotropin alfa, 36 mg Mannitol, 5.1 mg Sodium Phosphate, and 2.4 mg Sodium Chloride. | Lyophilized powder | IntramuSubcutaneousular preferably the buttocks | A 0.9 mg intramuscular injection to the buttock followed by a second 0.9 mg intramuscular injection to the buttock 24 hours later. | Allergic | Rash; hives; itching; difficulty breathing; tightness in the chest | Link | NA | NA |
| 10146 | Th1021 | Thyrotropin Alfa | >Th1021_Thyrotropin_Alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 | 25 ± 10 hours | Thyrotropin alfa is a recombinant form of thyroid stimulating hormone used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients. | For detection of residueal or recurrent thyroid cancer | Binding of thyrotropin alfa to TSH receptors on normal thyroid epithelial cells or on well-differentiated thyroid cancer tissue stimulates iodine uptake and organification. Thyrogen is an exogenous source of human TSH that offers an additional diagnostic tool in the follow-up of patients with a history of well-differentiated thyroid cancer. | Binding of thyrotropin Alfa to the thyrotropin receptors found on any residual thyroid cells or tissues stimulates radioactive iodine uptake for better radiodiagnostic imaging. | NA | NA | Time to peak: Median: 10 hours (range: 3-24 hours) After a single intramuscular injection of 0.9 mg of thyrotropin alfa: Cmax= 116+38mU/L, Tmax=22+8.5 hours. AUC=5088+1728 mU·hr/L. | NA | Through kidney and liver | Agents used to treat hypothyroidism, Anterior Pituitary Lobe Hormones and Analogues, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Pituitary and Hypothalamic Hormones and Analogues, Pituitary Hormones, Pituitary Hormones, Anterior, Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins, Thyroid Products | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Swelling of the mouth, face, lips, or tongue; confusion; one-sided weakness | Link | NA | NA |
| 10147 | Th1021 | Thyrotropin Alfa | >Th1021_Thyrotropin_Alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 | 25 ± 10 hours | Thyrotropin alfa is a recombinant form of thyroid stimulating hormone used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients. | For detection of residueal or recurrent thyroid cancer | Binding of thyrotropin alfa to TSH receptors on normal thyroid epithelial cells or on well-differentiated thyroid cancer tissue stimulates iodine uptake and organification. Thyrogen is an exogenous source of human TSH that offers an additional diagnostic tool in the follow-up of patients with a history of well-differentiated thyroid cancer. | Binding of thyrotropin Alfa to the thyrotropin receptors found on any residual thyroid cells or tissues stimulates radioactive iodine uptake for better radiodiagnostic imaging. | NA | NA | Time to peak: Median: 10 hours (range: 3-24 hours) After a single intramuscular injection of 0.9 mg of thyrotropin alfa: Cmax= 116+38mU/L, Tmax=22+8.5 hours. AUC=5088+1728 mU·hr/L. | NA | Through kidney and liver | Agents used to treat hypothyroidism, Anterior Pituitary Lobe Hormones and Analogues, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Pituitary and Hypothalamic Hormones and Analogues, Pituitary Hormones, Pituitary Hormones, Anterior, Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins, Thyroid Products | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Severe or persistent dizziness or headache; shortness of breath or other breathing problems; slurred speech; vision problems. | Link | NA | NA |
| 10215 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | Antagon (ganirelix) | Follicle-stimulating hormone receptor,Lutropin-choriogonadotropic hormone receptor | Menopur | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Menotropins are used to stimulate ovulation (the release of an egg) when a woman's ovaries can produce a follicle but hormonal stimulation is deficient. Menotropins are also used to stimulate the development of multiple eggs for in vitro fertilization. Li | NA | Each vial of MENOPUR contains 75 International Units of follicle-stimulating hormone (FSH) activity and 75 International Units of luteinizing hormone (LH) activity, plus 21 mg lactose monohydrate and 0.005 mg Polysorbate 20 and Sodium Phosphate Buffer (So | Sterile, lyophilized powder which is reconstitution with Sterile 0.9% Sodium Chloride Injection. | Subcutaneous Injection | The dosing scheme for patients undergoing IVF follows a stepwise approach and is individualized for each woman. The recommended initial dose of MENOPUR for women who have received a GnRH agonist for pituitary suppression is 225 International Units. MENOPU | Hypersensitivity, high level of FSH indicating primary ovarian failure, cause fetal harm when administerd to prergnant woman, ex hormone dependent tumors of the reproductive tract and accessory organs. | Less than 2% of female patients treated with menotropins develop ovarian hyperstimulation syndrome (OHSS), especially after the first cycle of therapy. Symptoms of OHSS include swelling of the hands or legs, abdominal pain and swelling, shortness of breathing. | Link | NA | NA |
| 10216 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | Follicle stimulating hormone / ganirelix | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Tumors of pituitary gland or hypothalamus and abnormal uterine bleeding of undetermined origin | Ovarian enlargement presenting as abdominal or pelvic pain, tenderness, pressure, or swelling; nausea, vomiting, or diarrhea; shortness of breath; pain, warmth, or tenderness centralized in an arm or leg; fever or chills. | Link | NA | NA |
| 10217 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | Follistim / Antagon (follicle stimulating hormone / ganirelix) | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Ovarian cyst or enlargement of undetermined origin, not due to polycystic ovary syndrome | Headache or drowsiness; weakness or aching of muscles or joints; breast enlargement or tenderness; pain, swelling, or irritation at the injection site; or rash. | Link | NA | NA |
| 10218 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | NA | Repronex | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Repronex is generally used as part of an assisted reproductive technology (ART) program to treat infertility in women. | NA | Each vial of Repronex (menotropins for injection) contains 75 International Units (IU) or 150 IU of follicle-stimulating hormone (FSH) activity and 75 IU or 150 IU of luteinizing hormone (LH) activity, respectively, plus 20 mg lactose monohydrate in a ste | Sterile, lyophilized form | Subcutaneous or intramuSubcutaneousular Injection. | The initial dose of Repronex (menotropins for injection) for patients who have received GnRH agonist or antagonist pituitary suppression is 150 IU daily for the first 5 days of treatment. Based on clinical monitoring (including serum estradiol levels and | A high FSH level indicating primary ovarian failure. | Rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); breast pain or enlarged breasts; calf, leg, or arm pain, swelling, redness, or tenderness; change in balance | Link | NA | NA |
| 10219 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | An organic intracranial lesion such as a pituitary tumor. | Change in color of skin to a bluish color (eg, on the lips, nail beds, fingers, toes); changes in speech or vision; chest, jaw, or arm pain; confusion; coughing up blood; fainting; fast breathing; fast heartbeat. | Link | NA | NA |
| 10220 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Ovarian cysts or enlargement not due to polycystic ovary syndrome. | Flu-like symptoms; one-sided weakness; pale skin; shortness of breath; sudden, severe nausea or vomiting; unusual sweating; weakness; yellowing of the skin or eyes. | Link | NA | NA |
| 10221 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Uncontrolled thyroid and adrenal dysfunction. | NA | NA | NA | NA |
| 10222 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | The presence of any cause of infertility other than anovulation unless they are candidates for in vitro-fertilization. | NA | NA | NA | NA |
| 10223 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Abnormal bleeding of undetermined origin. | NA | NA | NA | NA |
| 10224 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Prior hypersensitivity to menotropins | NA | NA | NA | NA |
| 10225 | Th1029 | Menotropins | >Th1029_Menotropins APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 23390.3 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | NA | Menotropins contains follicle stimulating hormone and luteinizing hormone purified from the urine of postmenopausal women. It is used as a fertility medication that is injected either subcutaneously or intramuscularly. It is composed of LH with 2 subunit alpha = 92 residues, beta = 121 residues and FSH with 2 subunits, alpha = 92 residues, beta=111 residues. | For the treatment of female infertility | Menotropins is used to treat female infertility, stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Menotropins bind to the LH/hCG/FSH receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Menotropins is a combination drug which binds to the Follicle stimulating hormone receptor (which results in ovulation in the absence of sufficient endogenous Luteinizing hormone)and it also binds to the LH receptor, thereby stimulating proper hormone release. The drug contains both FSH and LH,therefore, it induces ovarian follicular growth and development as well as gonadal steroid production in women who do not have ovarian failure.FSH is the primary driver of follicular recruitment and growth in early folliculogenesis, while LH is important for ovarian steroidogenesis and is involved in the physiological events leading to development of a competent pre-ovulatory follicle. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins, Biological Products, Complex Mixtures, Fertility Agents, Fertility Agents, Female, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Reproductive Control Agents, Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Repronex (menotropins for injection) is not indicated in women who are pregnant. There are limited human data on the effects of menotropins when administered during pregnancy. | NA | NA | NA | NA |
| 10269 | Th1039 | Lutropin alfa | >Th1039_Lutropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 30000 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | approximately 18 hours | Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein. Each monomeric unit is a glycoprotein molecule. In females, an acute rise of LH(LH surge) triggers ovulation and the development of the corpus luteum. In males, it stimulates Leydig cell production of testosterone. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. | For treatment of female infertility | Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone, which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. LH also induces the ovulated follicle to become a corpus luteum, which then secretes progesterone. | Binds to the luteinizing hormone receptor which then activates adenylate cylcase through G protein mediation. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes. | Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus. | <5% of dose excreted renally as unchanged drug. | bioavailability is 56% | 10 L | 2-3 L/h [healthy female following subcutaneous administration]. Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally. | Genito Urinary System and Sex Hormones, Gonadotropins | US5767251 | 16-Jun-1998 | 16-Jun-2015 | Other drugs may interact with lutropin alfa, including prescription and over-the-counter medicines, vitamins, and herbal products | Lutropin-choriogonadotropic hormone receptor | Luveris | Serono, Merck Europe B.V. | Serono, Merck Europe B.V. | Luveris is used together with follitropin alfa to treat infertility in women with LH deficiency. | NA | One vial contains 75 IU of lutropin alfa (recombinant human Luteinising Hormone {r-hLH}) and following excipeint is present; Powder:Sucrose,Disodium phosphate dihydrate,Sodium dihydrogen phosphate monohydrate,Polysorbate 20,Phosphoric acid, concentrated ( | White lyophilised pellet withg clear colourless solvent to make solution | Subcutaneous (Subcutaneous) administration | It is recommended that 75 IU Luveris be concomitantly administered subcutaneously with 75 IU to 150 IU Gonal-f as two separate injections in the initial treatment cycle | Hypersensitivity | Nausea, stomach pain, diarrhea, constipation, gas; pelvic pain, menstrual cramps; breast pain; headache; pain or irritation where the injection was given; tired feeling; or cold symptoms such as stuffy nose, sneezing, sore throat. | Link | NA | NA |
| 10270 | Th1039 | Lutropin alfa | >Th1039_Lutropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 30000 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | approximately 18 hours | Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein. Each monomeric unit is a glycoprotein molecule. In females, an acute rise of LH(LH surge) triggers ovulation and the development of the corpus luteum. In males, it stimulates Leydig cell production of testosterone. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. | For treatment of female infertility | Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone, which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. LH also induces the ovulated follicle to become a corpus luteum, which then secretes progesterone. | Binds to the luteinizing hormone receptor which then activates adenylate cylcase through G protein mediation. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes. | Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus. | <5% of dose excreted renally as unchanged drug. | bioavailability is 56% | 10 L | 2-3 L/h [healthy female following subcutaneous administration]. Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally. | Genito Urinary System and Sex Hormones, Gonadotropins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Tumours of the hypothalamus and pituitary gland | NA | Link | NA | NA |
| 10271 | Th1039 | Lutropin alfa | >Th1039_Lutropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 30000 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | approximately 18 hours | Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein. Each monomeric unit is a glycoprotein molecule. In females, an acute rise of LH(LH surge) triggers ovulation and the development of the corpus luteum. In males, it stimulates Leydig cell production of testosterone. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. | For treatment of female infertility | Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone, which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. LH also induces the ovulated follicle to become a corpus luteum, which then secretes progesterone. | Binds to the luteinizing hormone receptor which then activates adenylate cylcase through G protein mediation. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes. | Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus. | <5% of dose excreted renally as unchanged drug. | bioavailability is 56% | 10 L | 2-3 L/h [healthy female following subcutaneous administration]. Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally. | Genito Urinary System and Sex Hormones, Gonadotropins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Ovarian enlargement or ovarian cyst unrelated to polycystic ovarian disease and of unknown origin. | NA | NA | NA | NA |
| 10272 | Th1039 | Lutropin alfa | >Th1039_Lutropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 30000 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | approximately 18 hours | Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein. Each monomeric unit is a glycoprotein molecule. In females, an acute rise of LH(LH surge) triggers ovulation and the development of the corpus luteum. In males, it stimulates Leydig cell production of testosterone. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. | For treatment of female infertility | Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone, which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. LH also induces the ovulated follicle to become a corpus luteum, which then secretes progesterone. | Binds to the luteinizing hormone receptor which then activates adenylate cylcase through G protein mediation. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes. | Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus. | <5% of dose excreted renally as unchanged drug. | bioavailability is 56% | 10 L | 2-3 L/h [healthy female following subcutaneous administration]. Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally. | Genito Urinary System and Sex Hormones, Gonadotropins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Gynaecological haemorrhages of unknown origin | NA | NA | NA | NA |
| 10273 | Th1039 | Lutropin alfa | >Th1039_Lutropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 30000 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | approximately 18 hours | Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein. Each monomeric unit is a glycoprotein molecule. In females, an acute rise of LH(LH surge) triggers ovulation and the development of the corpus luteum. In males, it stimulates Leydig cell production of testosterone. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. | For treatment of female infertility | Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone, which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. LH also induces the ovulated follicle to become a corpus luteum, which then secretes progesterone. | Binds to the luteinizing hormone receptor which then activates adenylate cylcase through G protein mediation. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes. | Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus. | <5% of dose excreted renally as unchanged drug. | bioavailability is 56% | 10 L | 2-3 L/h [healthy female following subcutaneous administration]. Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally. | Genito Urinary System and Sex Hormones, Gonadotropins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Ovarian, uterine, or mammary carcinoma | NA | NA | NA | NA |
| 10274 | Th1039 | Lutropin alfa | >Th1039_Lutropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 30000 | C1014H1609N287O294S27 | 8.44 | -0.063 | 55 | approximately 18 hours | Lutropin alfa is a recombinant human luteinizing hormone produced in yeast with 2 subunits, alpha = 92 residues, beta = 121 residues. It is a heterodimeric glycoprotein. Each monomeric unit is a glycoprotein molecule. In females, an acute rise of LH(LH surge) triggers ovulation and the development of the corpus luteum. In males, it stimulates Leydig cell production of testosterone. Lutropin alfa was the first and only recombinant human form of luteinizing hormone (LH) developed for use in the stimulation of follicular development. | For treatment of female infertility | Used to facilitate female conception, lutropin alfa performs the same actions as luteinizing hormone, which is normally produced in the pituitary gland. Lutropin is usually given in combination with follitropin alfa. In females, a LH surge about halfway through the menstrual cycle triggers the onset of ovulation. LH also induces the ovulated follicle to become a corpus luteum, which then secretes progesterone. | Binds to the luteinizing hormone receptor which then activates adenylate cylcase through G protein mediation. Adenylate cyclase then activates many other pathways leading to steroid hormone production and other follicle maturation processes. | Lutropin alfa is not indicated for people under 16 and over 60, pregnant and lactating women, patients with uncontrolled thyroid and adrenal failure, patients with active, untreated tumours of the hypothalamus and pituitary gland, and in any patient with a condition that makes a normal pregnancy possible such as primary ovarian failure or fibroid tumors of the uterus. | <5% of dose excreted renally as unchanged drug. | bioavailability is 56% | 10 L | 2-3 L/h [healthy female following subcutaneous administration]. Total body clearance is approximately 2 to 3 L/h with less than 5 percent of the dose being excreted unchanged renally. | Genito Urinary System and Sex Hormones, Gonadotropins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Luveris must not be used when a condition exists which would make a normal pregnancy impossible, such as:primary ovarian failure, malformations of sexual organs incompatible with pregnancy, fibroid tumours of the uterus incompatible with pregnancy. | NA | NA | NA | NA |
| 10372 | Th1055 | Follitropin beta | >Th1055_Follitropin_beta APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin beta is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta†differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | For treatment of female infertility | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin alpha is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. | NA | bioavailability is approximately 66-76%. | 8 L [female subjects following intravenous administration of a 300 IU dose] | 0.011 /h/kg [European women with a single intramuscular dose of 300 IU] 0.011 /h/kg [Japanese women with a single intramuscular dose of 300 IU] | Amino Acids, Peptides, and Proteins, Follicle Stimulating Hormone, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Proteins, Sex Hormones and Modulators of the Genital System, Thyroid Products | US7741268 | 22-Jun-2010 | 2-Apr-2024 | NA | Follicle-stimulating hormone receptor | Follistim AQ | Merck | Merck | Follistim AQ (follitropin beta injection) is indicated for the development of multiple follicles in ovulatory patients participating in an Assisted Reproductive Technology (ART) program. Follistim AQ (follitropin beta) is also indicated for the induction of ovulation and pregnancy in anovulatory infertile patients in whom the cause of infertility is functional and not due to primary ovarian failure. | NA | Each single-use vial of Follistim AQ (follitropin beta) contains the following per 0.5 mL: 75 IU or 150 IU of FSH activity; 25 mg sucrose, NF; 7.35 mg sodium citrate (dihydrate), USP; 0.25 mg L-methionine, USP; 0.1 mg polysorbate 20, NF; and water for injection, USP. Hydrochloric acid, NF and/or sodium hydroxide, NF are used to adjust the pHto 7. | Follistim AQ (follitropin beta) is presented as a Sterile aqueous solution | for Subcutaneous or INTRAMUSubcutaneousULAR admini | starting dose of 150 to 225 IU of Follistim AQ (follitropin beta injection) is recommended for at least the first four days of treatment. After this, the dose may be adjusted for the individual patient based upon their ovarian response. | Tumor of the ovary, breast, uterus, hypothalamus or pituitary gland; Pregnancy; Uncontrolled thyroid or adrenal dysfunction; High levels of FSH indicating primary ovarian failure; | The following adverse events have been reported in women treated with gonado tropins: pulmonary and vascular complications, hemoperitoneum, adnexal torsion (as a complication of ovarian enlargement), dizziness, tachycardia, dyspnea, tachypnea, febrile reactions, flu-like symptoms including fever, chills, mus culoskeletal aches, joint pains, nausea, headache and malaise, breast tenderness, and dermatological symptoms | Link | NA | NA |
| 10373 | Th1055 | Follitropin beta | >Th1055_Follitropin_beta APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin beta is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta†differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | For treatment of female infertility | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin alpha is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. | NA | bioavailability is approximately 66-76%. | 8 L [female subjects following intravenous administration of a 300 IU dose] | 0.011 /h/kg [European women with a single intramuscular dose of 300 IU] 0.011 /h/kg [Japanese women with a single intramuscular dose of 300 IU] | Amino Acids, Peptides, and Proteins, Follicle Stimulating Hormone, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Proteins, Sex Hormones and Modulators of the Genital System, Thyroid Products | US5270057 | 14-Dec-1993 | 14-Dec-2010 | NA | NA | Bemfola | Gedeon Richter Plc | Gedeon Richter Plc | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10374 | Th1055 | Follitropin beta | >Th1055_Follitropin_beta APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin beta is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta†differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | For treatment of female infertility | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin alpha is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. | NA | bioavailability is approximately 66-76%. | 8 L [female subjects following intravenous administration of a 300 IU dose] | 0.011 /h/kg [European women with a single intramuscular dose of 300 IU] 0.011 /h/kg [Japanese women with a single intramuscular dose of 300 IU] | Amino Acids, Peptides, and Proteins, Follicle Stimulating Hormone, Genito Urinary System and Sex Hormones, Gonadotropins, Gonadotropins and Antigonadotropins, Gonadotropins, Pituitary, Hormones, Hormones, Hormone Substitutes, and Hormone Antagonists, Peptide Hormones, Peptides, Pituitary Hormones, Pituitary Hormones, Anterior, Proteins, Sex Hormones and Modulators of the Genital System, Thyroid Products | CA2037884 | 21-Oct-2003 | 8-Mar-2011 | NA | NA | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10440 | Th1077 | Urofollitropin | >Th1077_Urofollitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 980.162 | C42H65N11O12S2 | 7.5 | -0.33 | 55 | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Urofollitropin is a purified form of follicle-stimulating hormone (FSH) that is manufactured by extraction from human urine and then purified. It consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Urofollitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Urofollitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | For treatment of female infertility | Urofollitropin or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of urofollitropin is the primary hormone responsible for follicular recruitment and development. | FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | NA | NA | 0.74 | Time to peak in plasma: IM: 17 hours (single dose), 11 hours (multiple doses) SubQ: 21 hours (single dose), 10 hours (multiple doses) | NA | Fertility Agents | US5767067 | 16-Jun-1998 | 16-Jun-2015 | NA | Follicle-stimulating hormone receptor | BRAVELLE | Ferring Pharmaceuticals Inc. | Ferring Pharmaceuticals Inc. | BRAVELLE (urofollitropin for injection, purified) is a gonadotropin indicated for Induction of ovulation in women who have previously received pituitary suppression – intramuscular and subcutaneous administration, Development of multiple follicles as part of an Assisted Reproductive Technology (ART) cycle in ovulatory women who have previously received pituitary suppression | NA | Each vial of BRAVELLE contains 82.5 International Units (IU) of Follicle Stimulating Hormone (FSH) activity, 23 mg Lactose Monohydrate, 0.005 mg Polysorbate 20, and Sodium Phosphate buffer (Sodium Phosphate dibasic, Heptahydrate and Phosphoric acid) for pH adjustments, which, when reconstituted with diluent, will deliver 75 International Units of FSH. BRAVELLE contains up to 2% luteinizing hormone (LH) activity based on bioassay. Human Chorionic Gonadotropin(hCG) is not detected in BRAVELLE. When stored at 3° to 25, up to 40% of the α-subunits may be oxidized. | BRAVELLE is a sterile, lyophilized powder used after reconstitution with Sterile 0.9% Sodium Chloride Injection, USP | IntramuSubcutaneousular and Subcutaneous administr | Initial starting 150 International Units per day for 5 days, administered subcutaneously or intramuscularly in case of ovulation induction. In case of Assisted Reproductive Technology (ART) initial starting dose of the first cycle – 225 International Units per day for 5 days, administered subcutaneously. | RAVELLE is contraindicated in women who exhibits Prior hypersensitivity to BRAVELLE or urofollitropins, High levels of FSH indicating primary ovarian failure, Pregnancy, Presence of uncontrolled non-gonadal endocrinopathies, Sex hormone dependent tumors of the reproductive tract and accessory organ, Tumors of pituitary gland or hypothalamus, Abnormal uterine bleeding of undetermined origin, Ovarian cysts or enlargement of undetermined origin, not due to polycystic ovary syndrome. | The most common adverse reactions (≥5% incidence) in ovulation induction include: headache, hot flashes, OHSS, pain, and respiratory disorder. The most common adverse reactions (≥2% incidence) in ART include: abdominal cramps, abdominal fullness/enlargement, headache, nausea, OHSS, pain, pelvic pain, and post retrieval pain. | Link | NA | NA |
| 10441 | Th1077 | Urofollitropin | >Th1077_Urofollitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 980.162 | C42H65N11O12S2 | 7.5 | -0.33 | 55 | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Urofollitropin is a purified form of follicle-stimulating hormone (FSH) that is manufactured by extraction from human urine and then purified. It consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Urofollitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Urofollitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | For treatment of female infertility | Urofollitropin or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of urofollitropin is the primary hormone responsible for follicular recruitment and development. | FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | NA | NA | 0.74 | Time to peak in plasma: IM: 17 hours (single dose), 11 hours (multiple doses) SubQ: 21 hours (single dose), 10 hours (multiple doses) | NA | Fertility Agents | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Metrodin | NA | NA | Metrodin (urofollitropin for injection) and hCG given in a sequential manner are indicated for the stimulation of follicular development and the induction ofovulation in patients with polycystic ovary syndrome, and infertility, who have failed to respond or conceive following adequate clomiphene citrate therapy. Metrodin (urofollitropin for injection) and hCG may also be used to stimulate the development of multiple follicles in ovulatory patients undergoing Assisted Reproductive Technologies (ART) such as in vitro fertilization. | NA | Each ampule of Metrodin (urofollitropin for injection) contains 75 or 150 IU of follicle-stimulating hormone (FSH) activity, in not more than 0.83 mg (75 IU) or 1.66 mg (150 IU) of extract, plus 10 mg lactose | Metrodin (urofollitropin for injection) is a sterile, lypholized powder form contains an acidic, water soluble glycoprotein biologically standardized for FSH gonadotropin activity | IntramuSubcutaneousular Injection. | Initial starting 75 International Units per day for 5 days administered intramuscularly in polycystic ovary syndrome. In ART the dose is 150 IU per day. | contraindicated in High levels of FSH indicating primary ovarian failure, Uncontrolled thyroid or adrenal dysfunction, An organic intracranial lesion such as a pituitary tumor, The presence of any cause of infertility other than anovulation, as stated in the Indications unless they are candidates for Assisted Reproductive Technologies, Abnormal bleeding of undetermined origin, Ovarian cysts or enlargement of undetermined origin, Prior hypersensitivity to urofollitropin. | Pulmonary and vascular complications, Ovarian Hyperstimulation Syndrome, Adnexal torsion, Mild to moderate ovarian enlargement, Abdominal pain, Ovarian cysts, nausea, vomiting, diarrhea, abdominal cramps, bloating, Pain, rash, swelling, and/or irritation at the site of injection, Ectopic pregnancy, Congenital abnormalities, dry skin, body rash, hair loss, hives, Headache. | Link | NA | NA |
| 10442 | Th1077 | Urofollitropin | >Th1077_Urofollitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 980.162 | C42H65N11O12S2 | 7.5 | -0.33 | 55 | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Urofollitropin is a purified form of follicle-stimulating hormone (FSH) that is manufactured by extraction from human urine and then purified. It consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Urofollitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Urofollitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | For treatment of female infertility | Urofollitropin or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of urofollitropin is the primary hormone responsible for follicular recruitment and development. | FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | NA | NA | 0.74 | Time to peak in plasma: IM: 17 hours (single dose), 11 hours (multiple doses) SubQ: 21 hours (single dose), 10 hours (multiple doses) | NA | Fertility Agents | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertinex | NA | NA | FertinexTM (urofollitropin for injection, purified) and hCG given in a sequential manner are indicated for the stimulation of follicular recruitment and development and the induction of ovulation in patients with polycystic ovary syndrome and infertility, who have failed to respond or conceive following adequate clomiphene citrate therapy. Fertinex (urofollitropin) TM and hCG may also be used to stimulate the development of multiple follicles in ovulatory patients undergoing Assisted Reproductive Technologies (ART) such as in vitro fertilization. | NA | Each ampule of Fertinex (urofollitropin) TM contains either 75 IU or 150 IU of highly purified FSH and 10 mg lactose. If required, pH is adjusted with 0.1 M hydrochloric acid and/or 0.1 M sodium hydroxide. | Fertinex (urofollitropin) in asterile, lyophilized powder form contains an acidic, water soluble glycoprotein biologically standardized for FSH gonadotropin activity | Subcutaneous Injection. | Initial starting 75 International Units per day for 5 days administered intramuscularly in polycystic ovary syndrome. In ART the dose is 150 IU per day. | contraindicated in High levels of FSH indicating primary ovarian failure, Uncontrolled thyroid or adrenal dysfunction, An organic intracranial lesion such as a pituitary tumor, The presence of any cause of infertility other than anovulation, as stated in the Indications unless they are candidates for Assisted Reproductive Technologies, Abnormal bleeding of undetermined origin, Ovarian cysts or enlargement of undetermined origin, Prior hypersensitivity to urofollitropin. | Pulmonary and vascular complications, Ovarian Hyperstimulation Syndrome, Adnexal torsion, Mild to moderate ovarian enlargement, Abdominal pain, Ovarian cysts, nausea, vomiting, diarrhea, abdominal cramps, bloating, Pain, rash, swelling, and/or irritation at the site of injection, Ectopic pregnancy, Congenital abnormalities, dry skin, body rash, hair loss, hives, Headache. | Link | NA | NA |
| 10448 | Th1080 | Choriogonadotropin alfa | >Th1080_Choriogonadotropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25719.7 | C1105H1770N318O336S26 | 8.61 | -0.258 | 55 | Mean terminal half-life 29 ± 6 hr (initial half-life is 4.5± 0.5 hr) | Recombinant human chorionic gonadotropin with a 92-residue alpha subunit and a 145 residue beta subunit. Glycosylation consists of N-and O-linked carbohydrate moieties linked to N-52 and N-78 (on alpha subunit) and N13 and 30, S121, 127, 132 and 138 (on beta subunit). The primary structure of the alpha-chain of r-hCG is identical to that of the alpha-chain of hCG, FSH and LH. | For the treatment of female infertility | Choriogonadotropin alfa is used to treat female infertility, Choriogonadotropin alfa stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Ovidrel is an analogue of Luteinizing Hormone (LH) and binds to the LH/hCG receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Choriogonadotropin alfa binds to the Follicle stimulating hormone receptor which results in ovulation in the absence of sufficient endogenous Luteinizing hormone. | NA | NA | The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%. | 5.9 ± 1.0 L | 0.29 ± 0.04 L/h [healthy down-regulated females] | Genito Urinary System and Sex Hormones,Gonadotropins,Gonadotropins and Antigonadotropins,Sex Hormones and Modulators of the Genital System | US6706681 | 16-Mar-2004 | 16-Mar-2021 | NA | Lutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor | Choriogonadotropin alfa | Emd serono inc, Ferring pharmaceuticals inc, App pharmaceuticals llc, Bel mar laboratories inc, Bris | Emd serono inc, Ferring pharmaceuticals inc, App pharmaceuticals llc, Bel mar laboratories inc, Bris | NA | NA | Chorionic Gonadotropin for Injection, USP is available in multiple dose vials containing 10,000 USP Units with accompanying Bacteriostatic Water for Injection for reconstitution. When reconstituted with 10 mL of the accompanying diluent each vial contains: Chorionic Gonadotropin 10,000 Units, Mannitol 100 mg, Benzyl alcohol 0.9%, Water for Injection q.s. Buffered with dibasic sodium phosphate and monobasic sodium phosphate. Hydrochloric acid and/or sodium hydroxide may have been used for pH adjustment (6.0-8.0). Nitrogen gas is used in the freeze drying process. | NA | NA | Adult Dose for Ovulation Induction: Ovulation Induction (if the cause of anovulation is secondary and not due to primary ovarian failure): chorionic gonadotropin: 5000 to 10,000 units IM one day following last day of menotropins. recombinant chorionic gonadotropin: 250 mcg subcutaneously one day following last dose of follicle-stimulating agent. Usual Adult Dose for Hypogonadism - Male hypogonadotropic hypogonadism (secondary to a pituitary deficiency):500 to 1000 units IM three times a week for 3 weeks followed by the same dose twice a week for 3 weeks or, 4000 units IM three times a week for 6 to 9 months followed by 2000 units three times a week for an additional 3 months. | Nausea; pain, swelling, bruising, or redness at the injection site; vomiting. Severe allergic reactions, bloating or swelling in the stomach or pelvic area; breast pain; calf or leg pain, redness, swelling, or tenderness; chest pain; decreased urination; irregular heartbeat; persistent or severe nausea, vomiting, or diarrhea; severe pelvic pain; severe stomach pain or bloating; sudden shortness of breath; sudden, unexpected weight gain. The principal serious adverse reactions are: (1) Ovarian hyperstimulation, a syndrome of sudden ovarian enlargement, ascites with or without pain and/or pleural effusion, (2) Rupture of ovarian cysts with resultant hemoperitoneum, (3) Multiple births and (4) Arterial thromboembolism. Anaphylaxis and other hypersensitivity reactions have been reported with urinary-derived HCG products. | NA | NA | NA | NA |
| 10449 | Th1080 | Choriogonadotropin alfa | >Th1080_Choriogonadotropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25719.7 | C1105H1770N318O336S26 | 8.61 | -0.258 | 55 | Mean terminal half-life 29 ± 6 hr (initial half-life is 4.5± 0.5 hr) | Recombinant human chorionic gonadotropin with a 92-residue alpha subunit and a 145 residue beta subunit. Glycosylation consists of N-and O-linked carbohydrate moieties linked to N-52 and N-78 (on alpha subunit) and N13 and 30, S121, 127, 132 and 138 (on beta subunit). The primary structure of the alpha-chain of r-hCG is identical to that of the alpha-chain of hCG, FSH and LH. | For the treatment of female infertility | Choriogonadotropin alfa is used to treat female infertility, Choriogonadotropin alfa stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Ovidrel is an analogue of Luteinizing Hormone (LH) and binds to the LH/hCG receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Choriogonadotropin alfa binds to the Follicle stimulating hormone receptor which results in ovulation in the absence of sufficient endogenous Luteinizing hormone. | NA | NA | The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%. | 5.9 ± 1.0 L | 0.29 ± 0.04 L/h [healthy down-regulated females] | Genito Urinary System and Sex Hormones,Gonadotropins,Gonadotropins and Antigonadotropins,Sex Hormones and Modulators of the Genital System | US5767251 | 16-Jun-1998 | 16-Jun-2015 | NA | Lutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor | Ovitrelle | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10450 | Th1080 | Choriogonadotropin alfa | >Th1080_Choriogonadotropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25719.7 | C1105H1770N318O336S26 | 8.61 | -0.258 | 55 | Mean terminal half-life 29 ± 6 hr (initial half-life is 4.5± 0.5 hr) | Recombinant human chorionic gonadotropin with a 92-residue alpha subunit and a 145 residue beta subunit. Glycosylation consists of N-and O-linked carbohydrate moieties linked to N-52 and N-78 (on alpha subunit) and N13 and 30, S121, 127, 132 and 138 (on beta subunit). The primary structure of the alpha-chain of r-hCG is identical to that of the alpha-chain of hCG, FSH and LH. | For the treatment of female infertility | Choriogonadotropin alfa is used to treat female infertility, Choriogonadotropin alfa stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Ovidrel is an analogue of Luteinizing Hormone (LH) and binds to the LH/hCG receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Choriogonadotropin alfa binds to the Follicle stimulating hormone receptor which results in ovulation in the absence of sufficient endogenous Luteinizing hormone. | NA | NA | The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%. | 5.9 ± 1.0 L | 0.29 ± 0.04 L/h [healthy down-regulated females] | Genito Urinary System and Sex Hormones,Gonadotropins,Gonadotropins and Antigonadotropins,Sex Hormones and Modulators of the Genital System | US5767251 | 16-Jun-1998 | 16-Jun-2015 | NA | Lutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor | Ovidrel | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10451 | Th1080 | Choriogonadotropin alfa | >Th1080_Choriogonadotropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25719.7 | C1105H1770N318O336S26 | 8.61 | -0.258 | 55 | Mean terminal half-life 29 ± 6 hr (initial half-life is 4.5± 0.5 hr) | Recombinant human chorionic gonadotropin with a 92-residue alpha subunit and a 145 residue beta subunit. Glycosylation consists of N-and O-linked carbohydrate moieties linked to N-52 and N-78 (on alpha subunit) and N13 and 30, S121, 127, 132 and 138 (on beta subunit). The primary structure of the alpha-chain of r-hCG is identical to that of the alpha-chain of hCG, FSH and LH. | For the treatment of female infertility | Choriogonadotropin alfa is used to treat female infertility, Choriogonadotropin alfa stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Ovidrel is an analogue of Luteinizing Hormone (LH) and binds to the LH/hCG receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Choriogonadotropin alfa binds to the Follicle stimulating hormone receptor which results in ovulation in the absence of sufficient endogenous Luteinizing hormone. | NA | NA | The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%. | 5.9 ± 1.0 L | 0.29 ± 0.04 L/h [healthy down-regulated females] | Genito Urinary System and Sex Hormones,Gonadotropins,Gonadotropins and Antigonadotropins,Sex Hormones and Modulators of the Genital System | US5767251 | 16-Jun-1998 | 16-Jun-2015 | NA | Lutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor | Pregnyl | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10452 | Th1080 | Choriogonadotropin alfa | >Th1080_Choriogonadotropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25719.7 | C1105H1770N318O336S26 | 8.61 | -0.258 | 55 | Mean terminal half-life 29 ± 6 hr (initial half-life is 4.5± 0.5 hr) | Recombinant human chorionic gonadotropin with a 92-residue alpha subunit and a 145 residue beta subunit. Glycosylation consists of N-and O-linked carbohydrate moieties linked to N-52 and N-78 (on alpha subunit) and N13 and 30, S121, 127, 132 and 138 (on beta subunit). The primary structure of the alpha-chain of r-hCG is identical to that of the alpha-chain of hCG, FSH and LH. | For the treatment of female infertility | Choriogonadotropin alfa is used to treat female infertility, Choriogonadotropin alfa stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Ovidrel is an analogue of Luteinizing Hormone (LH) and binds to the LH/hCG receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Choriogonadotropin alfa binds to the Follicle stimulating hormone receptor which results in ovulation in the absence of sufficient endogenous Luteinizing hormone. | NA | NA | The mean absolute bioavailability following a single subcutaneous injection to healthy female volunteers is about 40%. | 5.9 ± 1.0 L | 0.29 ± 0.04 L/h [healthy down-regulated females] | Genito Urinary System and Sex Hormones,Gonadotropins,Gonadotropins and Antigonadotropins,Sex Hormones and Modulators of the Genital System | US5767251 | 16-Jun-1998 | 16-Jun-2015 | NA | Lutropin-choriogonadotropic hormone receptor,Follicle-stimulating hormone receptor | Chorionic Gonadotropin | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10507 | Th1099 | Mecasermin | >Th1099_Mecasermin GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA | 7649 | C331H518N94O101S7 | NA | NA | NA | 5.8 hours | E. coli derived, recombinant human insulin-like growth factor-1 (rhIGF-1). It has 70 amino acids in a single chain (identical to the endogenous human protein), with three intramolecular disulfide bridges and a molecular weight of 7649 daltons. | For the long-term treatment of growth failure in pediatric patients with Primary IGFD or with GH gene deletion who have developed neutralizing antibodies to GH. It is not indicated to treat Secondary IGFD resulting from GH deficiency, malnutrition, hypothyroidism or other causes; it is not a substitute for GH therapy. | Mecasermin is a biosynthetic (recombinant DNA origin) form of human insulin growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth. Growth hormones (GH) bind to growth hormone receptors (GHR) in the liver and other tissues, which stimulates the synthesis of IGF-1. In target tissues, IGF-1 activates the IGF-1 receptor, resulting in intracellular signals that stimulate growth. Although many actions of the GH are mediated through IGF-1, the precise roles of GH and IGF-1 have not been fully elucidated. Patients with severe primary IGF-1 deficiency (Primary IGFD) fail to produce adequate levels of IGF-1, due to disruption of the GH pathway used to promote IGF-1 release (possible GH pathway disruptions include mutations in the GHR, post-GHR signaling pathway, and IGF-1 gene defects). | Mecasermin supplies recombinant-DNA-origin IGF-1, which binds to the Type I IGF-1 receptor. This receptor exerts intra-cellular signaling activity in a number of processes involved in statural growth, including mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates, and increases in organ growth. | Overdosage of Mecasermin leads to hypoglycemia . One case of acute overdose was treated with IV glucose. Long-term overdosage may result in signs and symptoms of acromegaly. The effects of Mecasermin in human pregnancy has not been studied, however effects on fetal development in animal studies were only seen at doses higher than the maximum recommended human dose based on body surface area. Studies on excretion of the drug in human milk, use in patients under 2 years, use in patients over 65 years, or use in patients with renal or hepatic impairment have not been performed. | Information on the metabolism of Mecasermin is not readily available, however it is likely to be metabolized by the liver and kidney like other injectable peptide drugs | While the bioavailability of rhIGF-1 after subcutaneous administration in healthy subjects has been reported to be close to 100%, the absolute bioavailability of mecasermin given subcutaneously to subjects with primary insulin-like growth factor-1 deficiency (Primary IGFD) has not been determined. | 0.257 ± 0.073 L/kg [subjects with severe Primary IGFD] | Clearance of Mecasermin is inversely proportional to IGF binding protein 3 (IGFBP-3) * Clearance is estimated to be 0.04L/hr/kg at 0.5 micrograms/mL of IGFBP-3 * Clearance is estimated to be 0.01L/hr/kg at 3 micrograms/mL of IGFBP-3 (the median level of IGFBP-3 for patients with normal IGF-1 levels) | Amino Acids, Peptides, and Proteins,Anterior Pituitary Lobe Hormones and Analogues,Biological Factors,Blood Glucose Lowering Agents,Blood Proteins,Growth Substances,Hypoglycemia-Associated Agents,Intercellular Signaling Peptides and Proteins,Peptides,Pituitary and Hypothalamic Hormones and Analogues,Proteins,Somatomedins,Somatotropin Agonists,Somatropin and Somatropin Agonists,Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins | US5681814 | 28-Oct-1997 | 18-Sep-2017 | NA | Insulin-like growth factor 1 receptor,Insulin-like growth factor-binding protein 3,Insulin receptor,Cation-independent mannose-6-phosphate receptor | Increlex | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10508 | Th1099 | Mecasermin | >Th1099_Mecasermin GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA | 7649 | C331H518N94O101S8 | NA | NA | NA | 5.8 hours | E. coli derived, recombinant human insulin-like growth factor-1 (rhIGF-1). It has 70 amino acids in a single chain (identical to the endogenous human protein), with three intramolecular disulfide bridges and a molecular weight of 7649 daltons. | For the long-term treatment of growth failure in pediatric patients with Primary IGFD or with GH gene deletion who have developed neutralizing antibodies to GH. It is not indicated to treat Secondary IGFD resulting from GH deficiency, malnutrition, hypothyroidism or other causes; it is not a substitute for GH therapy. | Mecasermin is a biosynthetic (recombinant DNA origin) form of human insulin growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth. Growth hormones (GH) bind to growth hormone receptors (GHR) in the liver and other tissues, which stimulates the synthesis of IGF-1. In target tissues, IGF-1 activates the IGF-1 receptor, resulting in intracellular signals that stimulate growth. Although many actions of the GH are mediated through IGF-1, the precise roles of GH and IGF-1 have not been fully elucidated. Patients with severe primary IGF-1 deficiency (Primary IGFD) fail to produce adequate levels of IGF-1, due to disruption of the GH pathway used to promote IGF-1 release (possible GH pathway disruptions include mutations in the GHR, post-GHR signaling pathway, and IGF-1 gene defects). | Mecasermin supplies recombinant-DNA-origin IGF-1, which binds to the Type I IGF-1 receptor. This receptor exerts intra-cellular signaling activity in a number of processes involved in statural growth, including mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates, and increases in organ growth. | Overdosage of Mecasermin leads to hypoglycemia . One case of acute overdose was treated with IV glucose. Long-term overdosage may result in signs and symptoms of acromegaly. The effects of Mecasermin in human pregnancy has not been studied, however effects on fetal development in animal studies were only seen at doses higher than the maximum recommended human dose based on body surface area. Studies on excretion of the drug in human milk, use in patients under 2 years, use in patients over 65 years, or use in patients with renal or hepatic impairment have not been performed. | Information on the metabolism of Mecasermin is not readily available, however it is likely to be metabolized by the liver and kidney like other injectable peptide drugs | While the bioavailability of rhIGF-1 after subcutaneous administration in healthy subjects has been reported to be close to 100%, the absolute bioavailability of mecasermin given subcutaneously to subjects with primary insulin-like growth factor-1 deficiency (Primary IGFD) has not been determined. | 0.257 ± 0.073 L/kg [subjects with severe Primary IGFD] | Clearance of Mecasermin is inversely proportional to IGF binding protein 3 (IGFBP-3) * Clearance is estimated to be 0.04L/hr/kg at 0.5 micrograms/mL of IGFBP-3 * Clearance is estimated to be 0.01L/hr/kg at 3 micrograms/mL of IGFBP-3 (the median level of IGFBP-3 for patients with normal IGF-1 levels) | Amino Acids, Peptides, and Proteins,Anterior Pituitary Lobe Hormones and Analogues,Biological Factors,Blood Glucose Lowering Agents,Blood Proteins,Growth Substances,Hypoglycemia-Associated Agents,Intercellular Signaling Peptides and Proteins,Peptides,Pituitary and Hypothalamic Hormones and Analogues,Proteins,Somatomedins,Somatotropin Agonists,Somatropin and Somatropin Agonists,Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins | US5200509 | 6-Apr-1993 | 6-Apr-2010 | NA | Insulin-like growth factor 1 receptor,Insulin-like growth factor-binding protein 3,Insulin receptor,Cation-independent mannose-6-phosphate receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10562 | Th1113 | Glatiramer acetate | >Th1113_Glatiramer_acetate EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 5000-9000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate comprises acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, known to reduce the frequency of relapses in relapsing-remitting multiple sclerosis | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Copaxone | Teva Pharmaceutical Industries | Teva Pharmaceutical Industries | Glatiramer acetate, the active ingredient of COPAXONE, consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000 – 9,000 daltons. Glatiramer acetate is identified by specific antibodies. Chemically, glatiramer acetate is designated L-glutamic acid polymer with L-alanine, L-lysine and L-tyrosine, acetate (salt). | NA | Each 1 mL of COPAXONE solution contains 20 mg or 40 mg of glatiramer acetate and the following inactive ingredient: 40 mg of mannitol. The pH of the solutions is approximately 5.5 to 7.0. The biological activity of glatiramer acetate is determined by its ability to block the induction of experimental autoimmune encephalomyelitis (EAE) in mice. | Clear, colorless to slightly yellow, sterile, nonpyrogenic solution | Subcutaneous | COPAXONE is for subcutaneous use only. Do not administer intravenously. The dosing schedule depends on the product strength that is selected. The recommended doses are: COPAXONE 20 mg per mL: administer once per day or COPAXONE 40 mg per mL: administer three times per week and at least 48 hours apart. COPAXONE 20 mg per mL and COPAXONE 40 mg per mL are not interchangeable. | COPAXONE is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | most commonly associated with discontinuation were: injection site reactions, dyspnea, urticaria, vasodilatation, and hypersensitivity. The most common adverse reactions were: injection site reactions, vasodilatation, rash, dyspnea, and chest pain. | Link | NA | NA |
| 10563 | Th1114 | Preotact | >Th1114_Preotact SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hrs | Recombinant, pharmaceutical form of parathyroid hormone (PTH), which is a single-chain polypeptide composed of 84 amino acids. Its sequence is identical to the full-length native 84-amino acid PTH polypeptide. It lacks disulfide bonds and glycosylation sites. Preotact is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | Preotact | Nycomed | Nycomed | osteoporosis in women past menopause | NA | NA | NA | Subcutaneous | 100 micrograms given once a day. Your doctor may advise you to take supplementary calcium and vitamin D. | Do not use Preotact: if you are allergic (hypersensitive) to parathyroid hormone or any of the other ingredients of Preotact; if you have had radiation therapy to the skeleton; if you suffer from high calcium levels and other disturbances in the calcium-phosphor metabolism; if you have other bone disease (including hyperparathyroidism or Paget’s disease); if you have high levels of alkaline phosphatase; if you suffer from severe kidney problems; if you suffer from severe liver disease. | increased level of calcium in the blood, increased level of calcium in the urine, and nausea. back pain, constipation, decreased muscle strength, diarrhoea, dizziness, erythema at injection site, fast or irregular heart beats, headache, muscle cramps, pain in extremity, stomach upset, tiredness, and vomiting. | Link | NA | NA |
| 10666 | Th1144 | Follitropin alpha | >Th1144_Follitropin_alpha APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | NA | NA | 24-53 hours in females, 32-41 hours in males | Recombinant (CHO cell derived) human follicle stimulating hormone (FSH). It consists of two non-covalently linked, non-identical glycoproteins designated as the alpha (92 amino acids)- and beta (111 amino acids)- subunits. The alpha subunit is glycosylated at N51 and N78 while the beta subunit is glycosylated at N7 and N24. Follitropin alpha was the world's first recombinant human FSH preparation. The term “alpha†differentiates it from another recombinant human FSH product that was marketed later as follitropin beta. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate than beta but with significantly higher estradiol (E2) levels. The amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side-chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF) | The main pharmacodynamic parameters are serum inhibin, estradiol and total follicular volume with daily injections of follitropin. The quickest response was noticed with serum inhibin, which declined rapidly after discontinuation. Follicular growth showed late response and continued even after discontinuation of the drug and after decline of the serum concentrations. Thus follicular growth was better correlated with serum inhibin and estradiol rather than peal levels of the drug. It should be noted that there is great inter-individual variability | Follitropin is important for spermatogenesis, gonadal steroid production and follicule growth and maturation | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Gonal-F | Serono Laboratories | Serono Laboratories | induction of ovulation and pregnancy anovulatory infertile patients in whom the cause of infertility is functional and not due to primary ovarian failure, for the development of multiple follicles in the ovulatory patient participating in an Assisted Reproductive Technology (ART) program. | NA | Each Gonal-f (follitropin alfa) RFF single-dose vial is filled with 82 IU (6 µg)follitropin alfa to deliver 75 IU (5.5 µg) follitropin alfa and contains 30 mg sucrose, 1.11 mg dibasic sodium phosphate dihydrate, 0.45 mg monobasic sodium phosphate monohydrate, 0.1 mg methionine, and 0.05 mg polysorbate 20. Phosphoric acid and/or sodium hydroxide may be used prior to lyophilization for pH adjustment. Vials are reconstituted with Sterile Water for Injection, USP. | Gonal-f (follitropin alfa) RFF is a sterile, lyophilized powder intended for subcutaneous injection after reconstitution. | Subcutaneous Injection | 300 IU per day | Prior hypersensitivity to recombinant FSH preparations or one of their excipients, High levels of FSH indicating primary ovarian failure., Uncontrolled thyroid or adrenal dysfunction, An organic intracranial lesion such as a pituitary tumor, Abnormal uterine bleeding of undetermined origin, Ovarian cyst or enlargement of undetermined origin, Sex hormone dependent tumors of the reproductive tract and accessory organs, Pregnancy. | headache, ovarian cyst, nausea, and upper respiratory tract infection | Link | NA | NA |
| 10667 | Th1144 | Follitropin alpha | >Th1144_Follitropin_alpha APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | NA | NA | NA | Recombinant (CHO cell derived) human follicle stimulating hormone (FSH). It consists of two non-covalently linked, non-identical glycoproteins designated as the alpha (92 amino acids)- and beta (111 amino acids)- subunits. The alpha subunit is glycosylated at N51 and N78 while the beta subunit is glycosylated at N7 and N24. Follitropin alpha was the world's first recombinant human FSH preparation. The term “alpha†differentiates it from another recombinant human FSH product that was marketed later as follitropin beta. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate than beta but with significantly higher estradiol (E2) levels. The amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side-chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF) | The main pharmacodynamic parameters are serum inhibin, estradiol and total follicular volume with daily injections of follitropin. The quickest response was noticed with serum inhibin, which declined rapidly after discontinuation. Follicular growth showed late response and continued even after discontinuation of the drug and after decline of the serum concentrations. Thus follicular growth was better correlated with serum inhibin and estradiol rather than peal levels of the drug. It should be noted that there is great inter-individual variability | Follitropin is important for spermatogenesis, gonadal steroid production and follicule growth and maturation | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Gonal-f RFF | EMD SERONO | EMD SERONO | ovulation and pregnancy in the oligo-anovulatory infertile patient in whom the cause of infertility is functional and not due to primary ovarian failure, development of multiple follicles in the ovulatory patient participating in an Assisted Reproductive Technology (ART) program. | NA | Each Gonal-f RFF single-dose vial is filled with 82 IU (6 µg)follitropin alfa to deliver 75 IU (5.5 µg) follitropin alfa and contains 30 mg sucrose, 1.11 mg dibasic sodium phosphate dihydrate, 0.45 mg monobasic sodium phosphate monohydrate, 0.1 mg methionine, and 0.05 mg polysorbate 20. Phosphoric acid and/or sodium hydroxide may be used prior to lyophilization for pH adjustment. Vials are reconstituted with Sterile Water for Injection, USP. | Gonal-f RFF (follitropin alfa injection) is a sterile, lyophilized powder intended for subcutaneous injection after reconstitution. | Subcutaneous Injection | 300 IU per day | Prior hypersensitivity to recombinant FSH preparations or one of their excipients, High levels of FSH indicating primary ovarian failure., Uncontrolled thyroid or adrenal dysfunction, An organic intracranial lesion such as a pituitary tumor, Sex hormone dependent tumors of the reproductive tract and accessory organs, Abnormal uterine bleeding of undetermined origin, Ovarian cyst or enlargement of undetermined origin, Pregnancy. | Headache, Dizziness, Migraine, Abdominal Pain, Nausea, Flatulence, Diarrhea, Toothache, Dyspepsia, Constipation, Stomatitis Ulcerative, Ovarian Cyst, Reproductive, Female, Ovarian Hyperstimulation, Breast Pain Female, Vaginal Haemorrhage, Gynecological-related pain, Uterine haemorrhage, Sinusitis, Pharyngitis, Rhinitis, Coughing, Injection Site Pain, Injection Site Inflammation, Back Pain, Pain, Fever, Hot Flushes, Malaise, Acne, Micturition Frequency, Cystitis, Infection viral. | Link | NA | NA |
| 10695 | Th1158 | Aprotinin | >Th1158_Aprotinin RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA | 6511.439 | C284H432N84O79S7 | NA | NA | >100 | Plasma half life: 150 minutes, Elimination half life: 10hrs | Aprotinin, also known as bovine pancreatic trypsin inhibitor, BPTI (Trasylol, Bayer) is a protein, that is used as medication administered by injection to reduce bleeding during complex surgery, such as heart and liver surgery. Its main effect is the slowing down of fibrinolysis, the process that leads to the breakdown of blood clots. The aim in its use is to decrease the need for blood transfusions during surgery, as well as end-organ damage due to hypotension (low blood pressure) as a result of marked blood loss. | For prophylactic use to reduce perioperative blood loss and the need for blood transfusion in patients undergoing cardiopulmonary bypass in the course of coronary artery bypass graft surgery who are at an increased risk for blood loss and blood transfusion. | Aprotinin is a broad spectrum protease inhibitor which modulates the systemic inflammatory response (SIR) associated with cardiopulmonary bypass (CPB) surgery. SIR results in the interrelated activation of the hemostatic, fibrinolytic, cellular and humoral inflammatory systems. Aprotinin, through its inhibition of multiple mediators [e.g., kallikrein, plasmin] results in the attenuation of inflammatory responses, fibrinolysis, and thrombin generation. Aprotinin inhibits pro-inflammatory cytokine release and maintains glycoprotein homeostasis. In platelets, aprotinin reduces glycoprotein loss (e.g., GpIb, GpIIb/IIIa), while in granulocytes it prevents the expression of pro-inflammatory adhesive glycoproteins. | Aprotinin inhibits several serine proteases, specifically trypsin, chymotrypsin and plasmin at a concentration of about 125,000 IU/ml, and kallikrein at 300,000 IU/ml. Its action on kallikrein leads to the inhibition of the formation of factor XIIa. As a result, both the intrinsic pathway of coagulation and fibrinolysis are inhibited. Its action on plasmin independently slows fibrinolysis. | NA | Aprotinin is slowly degraded by lysosomal enzymes. | 100% (IV) | NA | NA | NA | US5198534 | NA | NA | Captopril- aprotinin infused intravenously in a dose of 2 million KIU over two hours blocked the acute hypotensive effect of 100mg of captopril. | Trypsin-1,Chymotrypsinogen B,Plasminogen,Kallikrein-1 | Trasylol | Bayer Pharmaceuticals | Bayer Pharmaceuticals | Trasylol (aprotinin) is indicated for prophylactic use to reduce perioperative blood loss and the need for blood transfusion in patients undergoing cardiopulmonary bypass in the course of coronary artery bypass graft surgery who are at an increased risk for blood loss and blood transfusion. | NA | Each milliliter contains 10,000 KIU (Kallikrein Inhibitor Units) (1.4 mg/mL) and 9 mg sodium chloride in water for injection. Hydrochloric acid and/or sodium hydroxide is used to adjust the pH to 4.5-6.5. | It is supplied as a clear, colorless, sterile isotonic solution | Intravenous administration | dosage is given as two regimens: Regimen A and Regimen B intial dose is same 1ml (1.4mg or 10000 KIU) but loading dose and PumpPrime dose is 200ml in case of regimen A and 100ml in case of regimen B, and constant infusion rate is 50ml/hr in A and 25ml/hr in B. | Administration of Trasylol (aprotinin) to patients with a known or suspected previous aprotinin exposure during the last 12 months is contraindicated. For patients with known or suspected history of exposure to aprotinin greater than 12 months previously. | Ventricular fibrillation, heart arrest, bradycardia, congestive heart failure, hemorrhage, bundle branch block, myocardial ischemia, ventricular tachycardia, heart block, pericardial effusion, ventricular arrhythmia, shock, pulmonary hypertension. Hyperglycemia, hypokalemia, hypervolemia, acidosis. Arthralgia. Agitation, dizziness, anxiety, convulsion. Pneumonia, apnea, increased cough, lung edema. | Link | NA | NA |
| 10696 | Th1158 | Aprotinin | >Th1158_Aprotinin RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA | 6511.439 | C284H432N84O79S7 | NA | NA | >100 | Plasma half life: 150 minutes, Elimination half life: 10hrs | NA | NA | NA | NA | NA | Aprotinin is slowly degraded by lysosomal enzymes. | 100% (IV) | NA | NA | NA | CA2030783 | NA | NA | Heparin- Aprotinin, in the presence of heparin, has been found to prolong the activated clotting time (ACT) as measured by a celite surface activation method | Trypsin-1,Chymotrypsinogen B,Plasminogen,Kallikrein-1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 10697 | Th1158 | Aprotinin | >Th1158_Aprotinin RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA | 6511.439 | C284H432N84O79S7 | NA | NA | >100 | Plasma half life: 150 minutes, Elimination half life: 10hrs | NA | NA | NA | NA | NA | Aprotinin is slowly degraded by lysosomal enzymes. | 100% (IV) | NA | NA | NA | NA | NA | NA | Tenecteplase- Aprotonin may antagonize the effect of Tenecteplase | Trypsin-1,Chymotrypsinogen B,Plasminogen,Kallikrein-1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 10698 | Th1158 | Aprotinin | >Th1158_Aprotinin RPDFCLEPPYTGPCKARIIRYFYNAKAGLCQTFVYGGCRAKRNNFKSAEDCMRTCGGA | 6511.439 | C284H432N84O79S7 | NA | NA | >100 | Plasma half life: 150 minutes, Elimination half life: 10hrs | NA | NA | NA | NA | NA | Aprotinin is slowly degraded by lysosomal enzymes. | 100% (IV) | NA | NA | NA | NA | NA | NA | Urokinase- Aprotonin may antagonize the effect of Urokinase | Trypsin-1,Chymotrypsinogen B,Plasminogen,Kallikrein-1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA |
| 10861 | Th1223 | Chorionic Gonadotropin (Human) | >Th1223_Chorionic_Gonadotropin_(Human) APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | Human chorionic gonadotropin (HCG), a polypeptide hormone produced by the human placenta. Endogenously produced HCG interacts with the LHCG receptor of the ovary and promotes the maintenance of the corpus luteum during the beginning of pregnancy. This allows the corpus luteum to continuously secrete the hormone progesterone during the first trimester, which is required for maintenance of the uterus and prevents menstruation. In males, HCG also stimulates the production of gonadal steroid hormones by stimulating the interstitial cells (Leydig cells) of the testis to produce androgens. HCG is composed of an alpha and a beta sub-unit. The alpha sub-unit is essentially identical to the alpha sub units of the human pituitary gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), as well as to the alpha sub-unit of human thyroid-stimulating hormone (TSH), while the beta sub units of these hormones differ in amino acid sequence. As a drug product, chorionic gonadotropin is a highly purified pyrogen-free preparation obtained from the urine of pregnant females. | For the treatment of prepubertal cryptorchidism (not due to anatomical obstruction), for the treatment of selected cases of hypogonadotropic hypogonadism (hypogonadism secondary to a pituitary deficiency) in males and for the induction of ovulation and pregnancy in the anovulatory, infertile woman in whom the cause of anovulation is secondary and not due to primary ovarian failure, and who has been appropriately pretreated with human menotropins. | he action of HCG is virtually identical to that of pituitary LH, although HCG appears to have a small degree of FSH activity as well. It stimulates production of gonadal steroid hormones by stimulating the interstitial cells (Leydig cells) of the testis to produce androgens and the corpus luteum of the ovary to produce progesterone. | NA | NA | NA | NA | NA | NA | Hormones | US6706681 | 16-03-2004 | 16-03-2021 | NA | Lutropin-choriogonadotropic hormone receptor | Ovidrel | Emd Serono | Emd Serono | It is indicated for the induction of final follicular maturation and early luteinization in infertile women who have undergone pituitary desensitization and who have been appropriately pretreated with follicle stimulating hormones as part of an Assisted Reproductive Technology (ART) program such as in vitro fertilization and embryo transfer. It is also indicated for the induction of ovulation (OI) and pregnancy in anovulatory infertile patients in whom the cause of infertility is functional and not due to primary ovarian failure. | NA | Each Ovidrel® PreFilled Syringe is filled with 0.515 mL containing 257.5 μg of choriogonadotropin alfa, 28.1 mg mannitol, 505 μg 85% O-phosphoric acid, 103 μg L-methionine, 51.5 μg Poloxamer 188, Sodium Hydroxide (for pH adjustment), and Water for Injection to deliver 250 μg of choriogonadotropin alfa in 0.5 mL. The pH of the solution is 6.5 to 7.5. | Injection, solution | Subcutaneous | Ovidrel® PreFilled Syringe 250 μg should be administered one day following the last dose of the follicle stimulating agent. Ovidrel® PreFilled Syringe should not be administered until adequate follicular development is indicated by serum estradiol and vaginal ultrasonography. | Ovidrel® PreFilled Syringe (choriogonadotropin alfa injection) is contraindicated in women who exhibit:Prior hypersensitivity to hCG preparations or one of their excipients.Primary ovarian failure.Uncontrolled thyroid or adrenal dysfunction.An uncontrolled organic intracranial lesion such as a pituitary tumor.Abnormal uterine bleeding of undetermined origin (see “Selection of Patientsâ€Â).Ovarian cyst or enlargement of undetermined origin (see “Selection of Patientsâ€Â).Sex hormone dependent tumors of the reproductive tract and accessory organs.Pregnancy. | Redness or pain at the injection site, mild abdominal pain, mood changes, or mild nausea/vomiting may occur. | Link | NA | NA |
| 10862 | Th1223 | Chorionic Gonadotropin (Human) | >Th1223_Chorionic_Gonadotropin_(Human) APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | Human chorionic gonadotropin (HCG), a polypeptide hormone produced by the human placenta. Endogenously produced HCG interacts with the LHCG receptor of the ovary and promotes the maintenance of the corpus luteum during the beginning of pregnancy. This allows the corpus luteum to continuously secrete the hormone progesterone during the first trimester, which is required for maintenance of the uterus and prevents menstruation. In males, HCG also stimulates the production of gonadal steroid hormones by stimulating the interstitial cells (Leydig cells) of the testis to produce androgens. HCG is composed of an alpha and a beta sub-unit. The alpha sub-unit is essentially identical to the alpha sub units of the human pituitary gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH), as well as to the alpha sub-unit of human thyroid-stimulating hormone (TSH), while the beta sub units of these hormones differ in amino acid sequence. As a drug product, chorionic gonadotropin is a highly purified pyrogen-free preparation obtained from the urine of pregnant females. | For the treatment of prepubertal cryptorchidism (not due to anatomical obstruction), for the treatment of selected cases of hypogonadotropic hypogonadism (hypogonadism secondary to a pituitary deficiency) in males and for the induction of ovulation and pregnancy in the anovulatory, infertile woman in whom the cause of anovulation is secondary and not due to primary ovarian failure, and who has been appropriately pretreated with human menotropins. | he action of HCG is virtually identical to that of pituitary LH, although HCG appears to have a small degree of FSH activity as well. It stimulates production of gonadal steroid hormones by stimulating the interstitial cells (Leydig cells) of the testis to produce androgens and the corpus luteum of the ovary to produce progesterone. | NA | NA | NA | NA | NA | NA | Hormones | US6706681 | 16-03-2004 | 16-03-2021 | NA | Lutropin-choriogonadotropic hormone receptor | Pregnyl | Physicians Total Care, Inc. | Physicians Total Care, Inc. | It is used for treating fertility problems in certain women who have not gone through menopause. Treating certain testicular development problems and stimulating the development of secondary sexual characteristics in certain patients. It is also used to treat boys 4 to 9 years old who have testicles that have not moved into the scrotum. | NA | Available in vials containing 10,000 USP units of sterile dried powder with 5 mg monobasic sodium phosphate and 4.4 mg dibasic sodium phosphate. If required, pH is adjusted with sodium hydroxide and/or phosphoric acid. Each package also contains a 10-mL vial of solvent containing: water for injection with 0.56% sodium chloride and 0.9% BENZYL ALCOHOL, WHICH IS NOT FOR USE IN NEWBORNS. If required, pH is adjusted with sodium hydroxide and/or hydrochloric acid. | Injection, Solution | Intramuscular, Subcutaneous | 4000 USP units 3 times weekly for 3 weeks. | Precocious puberty, prostatic carcinoma or other androgen-dependent neoplasm, prior allergic reaction to HCG. | Headache, irritability, restlessness, depression, fatigue, edema, precocious puberty, gynecomastia, pain at the site of injection. | Link | NA | NA |
| 10863 | Th1224 | Chorionic Gonadotropin (Recombinant) | >Th1224_Chorionic_Gonadotropin_(Recombinant) APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25719.7 | C1105H1770N318O336S26 | 8.61 | -0.258 | 55 °C | The mean terminal half-life is about 29 ± 6 hours (initial half-life is 4.5 ± 0.5 hours). | Recombinant human chorionic gonadotropin with 2 subunits, alpha = 92 residues, beta = 145 residues, each with N-and O-linked carbohydrate moieties linked to ASN-52 and ASN-78 (on alpha subunit) and ASN-13, ASN-30, SER-121, SER-127, SER-132 and SER-138 (on beta subunit). The primary structure of the alpha-chain of r-hCG is identical to that of the alpha-chain of hCG, FSH and LH. | For the treatment of female infertility | Choriogonadotropin alfa is used to treat female infertility, Choriogonadotropin alfa stimulates late follicular maturation and resumption of oocyte meiosis, and initiates rupture of the pre-ovulatory ovarian follicle. Ovidrel is an analogue of Luteinizing Hormone (LH) and binds to the LH/hCG receptor of the granulosa and theca cells of the ovary to effect these changes in the absence of an endogenous LH surge. | Choriogonadotropin alfa binds to the Follicle stimulating hormone receptor which results in ovulation in the absence of sufficient endogenous Luteinizing hormone. | NA | NA | NA | NA | NA | Hormones | US5767251 | 16-06-1998 | 16-06-2015 | NA | Lutropin-choriogonadotropic hormone receptor, Follicle-stimulating hormone receptor | Ovitrelle | Merck Serono Europe Limited | Merck Serono Europe Limited | Ovitrelle is indicated in the treatment of:women undergoing superovulation prior to assisted reproductive techniques such as in vitro fertilisation (IVF): Ovitrelle is administered to trigger final follicular maturation and luteinisation after stimulation of follicular growth;anovulatory or oligo-ovulatory women: Ovitrelle is administered to trigger ovulation and luteinisation in anovulatory or oligo-ovulatory patients after stimulation of follicular growth. | NA | Each pre-filled syringe contains 250 micrograms choriogonadotropin alfa* (equivalent to approximately 6,500 IU) in 0.5 mL solution | powder and solvent to be made up into a solution | Subcutaneous | One pre-filled syringe of Ovitrelle (250 micrograms) is administered 24 to 48 hours after the last administration of a follicle stimulating hormone (FSH) or human menopausal gonadotropin (hMG) preparation, i.e. when optimal stimulation of follicular growth is achieved. | hypersensitive (allergic) to choriogonadotropin alfa or any of the other ingredients. | The most common side effects with Ovitrelle (seen in between 1 and 10 patients in 100) are reactions at the injection site, headache, tiredness, vomiting, nausea (feeling sick), abdominal pain (stomach ache) and ovarian hyperstimulation syndrome (such as feeling sick, weight gain and diarrhoea). Ovarian hyperstimulation syndrome occurs when the ovaries over respond to treatment, especially when medicines to trigger ovulation have been used. | Link | NA | NA |
| 11631 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Amino Acids, Peptides, and Proteins | 5270057 | 14-12-1993 | 20-03-2011 | Fluvoxamine,Citalopram,Fluoxetine,Duloxetine,Trazodone,Paroxetine,Sertraline,Sibutramine,Nefazodone,Escitalopram,Zimelidine,Dapoxetine,Milnacipran,Desvenlafaxine,Seproxetine,Levomilnacipran,Indalpine,Ritanserin,Alaproclate,Amphetamine,Phentermine,Midodrine,Norepinephrine,Phenylephrine,Phenylpropanolamine,Metaraminol,Epinephrine,Methoxamine,Orciprenaline,Phenmetrazine,Dobutamine,Pseudoephedrine,Benzphetamine,Ritodrine,Terbutaline,Oxymetazoline,Diethylpropion,Dopamine,Isoprenaline,Lisdexamfetamine,Fenoterol,Ephedrine,Mephentermine,Procaterol,Clenbuterol,MMDA,Midomafetamine,2,5-Dimethoxy-4-ethylamphetamine,4-Bromo-2,5-dimethoxyamphetamine,Tenamfetamine,Chlorphentermine,Methylenedioxyethamphetamine,Dextroamphetamine,Metamfetamine,Nylidrin,Tetryzoline,Tyramine,Isoxsuprine,Etilefrine,Synephrine,Iofetamine I-123,Racepinephrine,Ritobegron,Tramazoline,Mephedrone,Fenozolone,Methoxyphenamine,Tretoquinol,Gepefrine,Prenalterol,Mefenorex,2,5-Dimethoxy-4-ethylthioamphetamine,Labetalol,Acebutolol,Celiprolol,Bucindolol,Epanolol,Gefitinib,Sorafenib,Erlotinib,Imatinib,Dasatinib,Lapatinib,Sunitinib,Genistein,3-[4-(1-formylpiperazin-4-yl)-benzylidenyl]-2-indolinone,Geldanamycin,PD173955,Radicicol,Cediranib,Nilotinib,Vatalanib,Vandetanib,Canertinib,Tandutinib,Motesanib,Dovitinib,Glesatinib,Lestaurtinib,Pazopanib,Midostaurin,Bosutinib,Axitinib,Piceatannol,Crizotinib,Cabozantinib,Ruxolitinib,Vemurafenib,Regorafenib,Ponatinib,Afatinib,Ibrutinib,Ceritinib,Lenvatinib,Nintedanib,Osimertinib,Alectinib,Selumetinib,Pacritinib,Acalabrutinib,Icotinib,Saracatinib,Neratinib,Crenolanib,Flumatinib,Dacomitinib,Tesevatinib,Entrectinib,Fostamatinib,Savolitinib,Gilteritinib,Erdafitinib,Brigatinib,Foretinib,Radotinib,Larotrectinib,Pexidartinib,Fedratinib,Tucatinib,Capmatinib,Selpercatinib,Tepotinib,Tivozanib,Infigratinib,Interferon alfa,Aldesleukin,Lovastatin,Ethionamide,Diazepam,Perphenazine,Metoclopramide,Perphenazine enanthate,Aminosalicylic acid,Resorcinol,Glimepiride,Acetohexamide,Chlorpropamide,Tolazamide,Glyburide,Glipizide,Gliclazide,Tolbutamide,Gliquidone,Glisoxepide,Glibornuride,Carbutamide,Metahexamide,Nortriptyline,Amitriptyline,Protriptyline,Imipramine,Amoxapine,Trimipramine,Doxepin,Desipramine,Clomipramine,Amineptine,Dimetacrine,Butriptyline,Dosulepin,Tianeptine,Oxaprotiline,Opipramol,Amitriptylinoxide,Dibenzepin,Quinupramine,Melitracen,Lofepramine,Iprindole,Imipramine oxide,Estetrol,Avapritinib,Naphazoline | Follicle-stimulating hormone receptor | Bemfola | Gedeon Richter Plc. | Gedeon Richter Plc. | Subcutaneous | 75 IU/0.125ml | NA | The most common side effects with Bemfola (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. For the full list of all side effects reported with Bemfola, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11632 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Chorionic Gonadotropin | 2037884 | 21-10-2003 | 08-03-2011 | NA | Follicle-stimulating hormone receptor | Bemfola | Gedeon Richter Plc. | Gedeon Richter Plc. | Subcutaneous | 150 IU/0.25ml | NA | The most common side effects with Bemfola (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. For the full list of all side effects reported with Bemfola, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11633 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Follicle Stimulating Hormone | 7563763 | 21-07-2009 | 23-08-2019 | NA | Follicle-stimulating hormone receptor | Bemfola | Gedeon Richter Plc. | Gedeon Richter Plc. | Subcutaneous | 225 IU/0.375ml | NA | The most common side effects with Bemfola (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. For the full list of all side effects reported with Bemfola, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11634 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Genito Urinary System and Sex Hormones | 5929028 | 27-07-1999 | 14-01-2018 | NA | Follicle-stimulating hormone receptor | Bemfola | Gedeon Richter Plc. | Gedeon Richter Plc. | Subcutaneous | 300 IU/0.50ml | NA | The most common side effects with Bemfola (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. For the full list of all side effects reported with Bemfola, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11635 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Gonadotropins | 7446090 | 04-11-2008 | 23-08-2019 | NA | Follicle-stimulating hormone receptor | Bemfola | Gedeon Richter Plc. | Gedeon Richter Plc. | Subcutaneous | 450 IU/0.75ml | NA | The most common side effects with Bemfola (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. For the full list of all side effects reported with Bemfola, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11636 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Gonadotropins and Antigonadotropins | 7741268 | 22-06-2010 | 02-04-2024 | NA | Follicle-stimulating hormone receptor | Bemfola Needles | Gedeon Richter Plc. | Gedeon Richter Plc. | Subcutaneous | 150 IU/0.25ml | NA | The most common side effects with Bemfola (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. | Bemfola is a medicine that contains the active substance follitropin alfa. It is used to treat the following groups: | Bemfola is available as a solution for injection in a prefilled pen. The medicine can only be obtained with a prescription and treatment should be started under the supervision of a doctor who has experience in the treatment of fertility problems | NA | NA | Link | Link | NA |
| 11637 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Gonadotropins, Pituitary | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Bravelle | Ferring Pharmaceuticals Inc. | Ferring Pharmaceuticals Inc. | Subcutaneous | 75 [iU]/1mL | BRAVELLE® is contraindicated in women who exhibit: Prior hypersensitivity to BRAVELLE® or urofollitropins High levels of FSH indicating primary ovarian failure [see INDICATIONS AND USAGE] Pregnancy BRAVELLE® may cause fetal harm when administered to a pregnant woman [see Use In Specific Populations]. BRAVELLE® is contraindicated in women who are pregnant. If this drug is used during pregnancy, or if the woman becomes pregnant while taking this drug, the woman should be apprised of the potential hazard to a fetus. Presence of uncontrolled non-gonadal endocrinopathies (e.g., thyroid, adrenal, or pituitary disorders) [see INDICATIONS AND USAGE] Sex hormone dependent tumors of the reproductive tract and accessory organ Tumors of pituitary gland or hypothalamus Abnormal uterine bleeding of undetermined origin Ovarian cysts or enlargement of undetermined origin, not due to polycystic ovary syndrome | headache, nausea, vomiting, mild stomach/abdominal pain, bloating, mild pelvic pain, cramps, constipation, injection site reactions (redness, pain, swelling, itching, or irritation), breast tenderness/pain, skin rash, hot flashes, or acne | Bravelle is a purified form of a hormone called follicle-stimulating hormone (FSH). This hormone is important in the development of follicles (eggs) that are produced by the ovaries in women. Bravelle is used together with other medicines to treat infertility in women with FSH deficiency. This medicine... | Bravelle is a prescription medicine used to treat the symptoms of Ovulation Induction, Assisted Reproductive Technology (ART), and Spermatogenesis. Bravelle may be used alone or with other medications. | NA | BRAVELLE® is a product containing a highly purified preparation of human follicle stimulating hormone (hFSH) extracted from the urine of postmenopausal women. Human FSH is a gonadotropin and consists of two non-covalently linked glycoproteins designated as the α and β subunits. The α subunit has 92 amino acids of which two are modified by attachment of carbohydrates. The β subunit has 111 amino acids of which two are modified by attachment of carbohydrates. | Link | Link | NA |
| 11638 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Hormones | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Intramuscular; Subcutaneous | 50 IU/0.5mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11639 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Hormones, Hormone Substitutes, and Hormone Antagonists | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Intramuscular; Subcutaneous | 75 IU/0.5mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11640 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Peptide Hormones | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Intramuscular; Subcutaneous | 100 IU/0.5mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11641 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Peptides | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Intramuscular; Subcutaneous | 150 IU/0.5mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11642 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Pituitary Hormones | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Intramuscular; Subcutaneous | 200 IU/0.5mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11643 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Pituitary Hormones, Anterior | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Subcutaneous | 150 IU/0.18mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11644 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Placental Hormones | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Subcutaneous | 300 IU/0.36mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11645 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Pregnancy Proteins | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Subcutaneous | 600 IU/0.72mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11646 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Proteins | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Fertavid | Merck Sharp & Dohme B.V. | Merck Sharp & Dohme B.V. | Subcutaneous | 900 IU/1.08mL | NA | NA | NA | NA | NA | NA | Link | Link | NA |
| 11647 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Follistim | Organon USA, Inc. | Organon USA, Inc. | Intramuscular; Subcutaneous | NA | Follistim® AQ (follitropin beta injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant hFSH products. High levels of FSH indicating primary ovarian failure. Uncontrolled thyroid or adrenal dysfunction. Tumor of the ovary, breast, uterus, hypothalamus or pituitary gland. Pregnancy. Heavy or irregular vaginal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome (PCOS). Hypersensitivity reactions to streptomycin or neomycin. Follistim® AQ (follitropin beta) may contain traces of these antibiotics and may cause hypersensitivity reactions in susceptible persons. | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Follistim AQ is a man-made form of a hormone that occurs naturally in the body. This hormone regulates ovulation, the growth and development of eggs in a woman's ovaries. Follistim AQ is used to treat infertility in women who cannot ovulate. This medicine is not effective in women with primary ovarian... | Follistim is a prescription medicine used to treat infertility in women to induce Ovulation and to stimulate sperm production in men (Spermatogenesis). Follistim may be used alone or with other medications. | NA | FOR SUBCUTANEOUS OR INTRAMUSCULAR USE ONLY | Link | Link | NA |
| 11648 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | Thyroid Products | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Follistim AQ | Organon USA, Inc. | Organon USA, Inc. | Subcutaneous | 175 [iU]/0.210mL | Follistim® AQ (follitropin beta injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant hFSH products. High levels of FSH indicating primary ovarian failure. Uncontrolled thyroid or adrenal dysfunction. Tumor of the ovary, breast, uterus, hypothalamus or pituitary gland. Pregnancy. Heavy or irregular vaginal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome (PCOS). Hypersensitivity reactions to streptomycin or neomycin. Follistim® AQ (follitropin beta) may contain traces of these antibiotics and may cause hypersensitivity reactions in susceptible persons. | The following adverse events have been reported in women treated with gonado tropins: pulmonary and vascular complications, hemoperitoneum, adnexal torsion (as a complication of ovarian enlargement), dizziness, tachycardia, dyspnea, tachypnea, febrile reactions, flu-like symptoms including fever, chills, mus culoskeletal aches, joint pains, nausea, headache and malaise, breast tenderness, and dermatological symptoms | NA | NA | NA | NA | Link | Link | NA |
| 11649 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Follistim AQ | Organon USA Inc. | Organon USA Inc. | Subcutaneous | 350 [iU]/0.42mL | Follistim® AQ (follitropin beta injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant hFSH products. High levels of FSH indicating primary ovarian failure. Uncontrolled thyroid or adrenal dysfunction. Tumor of the ovary, breast, uterus, hypothalamus or pituitary gland. Pregnancy. Heavy or irregular vaginal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome (PCOS). Hypersensitivity reactions to streptomycin or neomycin. Follistim® AQ (follitropin beta) may contain traces of these antibiotics and may cause hypersensitivity reactions in susceptible persons. | The following adverse events have been reported in women treated with gonado tropins: pulmonary and vascular complications, hemoperitoneum, adnexal torsion (as a complication of ovarian enlargement), dizziness, tachycardia, dyspnea, tachypnea, febrile reactions, flu-like symptoms including fever, chills, mus culoskeletal aches, joint pains, nausea, headache and malaise, breast tenderness, and dermatological symptoms | NA | NA | NA | NA | Link | Link | NA |
| 11650 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Follistim AQ | Organon USA Inc. | Organon USA Inc. | Subcutaneous | 650 [iU]/0.78mL | Follistim® AQ (follitropin beta injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant hFSH products. High levels of FSH indicating primary ovarian failure. Uncontrolled thyroid or adrenal dysfunction. Tumor of the ovary, breast, uterus, hypothalamus or pituitary gland. Pregnancy. Heavy or irregular vaginal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome (PCOS). Hypersensitivity reactions to streptomycin or neomycin. Follistim® AQ (follitropin beta) may contain traces of these antibiotics and may cause hypersensitivity reactions in susceptible persons. | The following adverse events have been reported in women treated with gonado tropins: pulmonary and vascular complications, hemoperitoneum, adnexal torsion (as a complication of ovarian enlargement), dizziness, tachycardia, dyspnea, tachypnea, febrile reactions, flu-like symptoms including fever, chills, mus culoskeletal aches, joint pains, nausea, headache and malaise, breast tenderness, and dermatological symptoms | NA | NA | NA | NA | Link | Link | NA |
| 11651 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Follistim AQ | Organon USA Inc. | Organon USA Inc. | Subcutaneous | 975 [iU]/1.17mL | Follistim® AQ (follitropin beta injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant hFSH products. High levels of FSH indicating primary ovarian failure. Uncontrolled thyroid or adrenal dysfunction. Tumor of the ovary, breast, uterus, hypothalamus or pituitary gland. Pregnancy. Heavy or irregular vaginal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome (PCOS). Hypersensitivity reactions to streptomycin or neomycin. Follistim® AQ (follitropin beta) may contain traces of these antibiotics and may cause hypersensitivity reactions in susceptible persons. | The following adverse events have been reported in women treated with gonado tropins: pulmonary and vascular complications, hemoperitoneum, adnexal torsion (as a complication of ovarian enlargement), dizziness, tachycardia, dyspnea, tachypnea, febrile reactions, flu-like symptoms including fever, chills, mus culoskeletal aches, joint pains, nausea, headache and malaise, breast tenderness, and dermatological symptoms | NA | NA | NA | NA | Link | Link | NA |
| 11652 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Follistim AQ | Organon USA Inc. | Organon USA Inc. | Intramuscular; Subcutaneous | 75 [iU]/0.5mL | Follistim® AQ (follitropin beta injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant hFSH products. High levels of FSH indicating primary ovarian failure. Uncontrolled thyroid or adrenal dysfunction. Tumor of the ovary, breast, uterus, hypothalamus or pituitary gland. Pregnancy. Heavy or irregular vaginal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome (PCOS). Hypersensitivity reactions to streptomycin or neomycin. Follistim® AQ (follitropin beta) may contain traces of these antibiotics and may cause hypersensitivity reactions in susceptible persons. | The following adverse events have been reported in women treated with gonado tropins: pulmonary and vascular complications, hemoperitoneum, adnexal torsion (as a complication of ovarian enlargement), dizziness, tachycardia, dyspnea, tachypnea, febrile reactions, flu-like symptoms including fever, chills, mus culoskeletal aches, joint pains, nausea, headache and malaise, breast tenderness, and dermatological symptoms | NA | NA | NA | NA | Link | Link | NA |
| 11653 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Follistim AQ | Organon USA Inc. | Organon USA Inc. | Intramuscular; Subcutaneous | 150 [iU]/0.5mL | Follistim® AQ (follitropin beta injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant hFSH products. High levels of FSH indicating primary ovarian failure. Uncontrolled thyroid or adrenal dysfunction. Tumor of the ovary, breast, uterus, hypothalamus or pituitary gland. Pregnancy. Heavy or irregular vaginal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome (PCOS). Hypersensitivity reactions to streptomycin or neomycin. Follistim® AQ (follitropin beta) may contain traces of these antibiotics and may cause hypersensitivity reactions in susceptible persons. | The following adverse events have been reported in women treated with gonado tropins: pulmonary and vascular complications, hemoperitoneum, adnexal torsion (as a complication of ovarian enlargement), dizziness, tachycardia, dyspnea, tachypnea, febrile reactions, flu-like symptoms including fever, chills, mus culoskeletal aches, joint pains, nausea, headache and malaise, breast tenderness, and dermatological symptoms | NA | NA | NA | NA | Link | Link | NA |
| 11654 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | EMD Serono, Inc. | EMD Serono, Inc. | Subcutaneous | 450 [iU]/1mL | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11655 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | EMD Serono, Inc. | EMD Serono, Inc. | Subcutaneous | 1050 [iU]/2mL | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11656 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular; Subcutaneous | 5.5 mcg / vial | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11657 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular; Subcutaneous | 33 mcg / vial | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11658 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular; Subcutaneous | 77 mcg / vial | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11659 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular; Subcutaneous | 75 unit / vial | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11660 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular; Subcutaneous | 150 unit / vial | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11661 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular; Subcutaneous | 37.5 unit / vial | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11662 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular; Subcutaneous | 1200 unit / vial | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11663 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | 75 IU | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11664 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | 1050 IU/1.75ml | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11665 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | 450 IU/0.75ml | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11666 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | 300 IU/0.5ml | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11667 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | 300 IU/0.5ml | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11668 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | 450 IU/0.75ml | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11669 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | 900 IU/1.5ml | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11670 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | 150 IU/0.25ml | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | headache, nausea, vomiting, mild stomach/abdominal pain, pelvic pain or tenderness, bloating, injection site reactions (redness, pain, bruising, irritation), breast swelling/tenderness/pain, numbness or tingly feeling, runny or stuffy nose, sore throat, acne, or skin rash. | NA | Gonal-F is indicated for: | NA | in women: | Link | Link | NA |
| 11671 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F Pen | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Subcutaneous | 900 unit / 1.5 mL | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11672 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F Pen | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Subcutaneous | 450 unit / 0.75 mL | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11673 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F Pen | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Subcutaneous | 300 unit / 0.5 mL | GONAL-F is contraindicated in women and men who exhibit:Prior hypersensitivity to recombinant FSH products or one of their excipients. Reactions have included anaphylaxis [see WARNINGS AND PRECAUTIONS]High levels of FSH indicating primary gonadal failureThe presence of uncontrolled non-gonadal endocrinopathies (for example, thyroid, adrenal, or pituitary disorders)Sex hormone dependent tumors of the reproductive tract and accessory organsTumors of pituitary gland or hypothalamusGONAL-F is also contraindicated in women who exhibit:Abnormal uterine bleeding of undetermined originOvarian cyst or enlargement of undetermined origin | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11674 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-F Rff | EMD Serono, Inc. | EMD Serono, Inc. | Subcutaneous | 75 [iU]/1mL | Gonal-f® RFF (follitropin alfa for injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant FSH preparations or one of their excipients. High levels of FSH indicating primary gonadal failure. Uncontrolled thyroid or adrenal dysfunction. Sex hormone dependent tumors of the reproductive tract and accessory organs. An organic intracranial lesion such as a pituitary tumor. Abnormal uterine bleeding of undetermined origin (see "Selection of Patients"). Ovarian cyst or enlargement of undetermined origin (see "Selection of Patients"). Pregnancy. | headache nausea vomiting mild stomach or abdominal pain bloating injection site reactions (pain, bruising, redness, or irritation) breast swelling/tenderness/pain numbness or tingly feeling, pelvic pain/tenderness/discomfort runny or stuffy nose sore throat acne or skin rash, | NA | Gonal-f RFF (follitropin alfa for injection) is a prescription medicine used to treat the symptoms of Ovulation Induction and Assisted Reproductive Technologies. Gonal-f RFF may be used alone or with other medications. | NA | Gonal-f® RFF (follitropin alfa for injection) is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the α- and β-subunits. The α- and β-subunits have 92 and 111 amino acids, respectively, and their primary and tertiary structure are indistinguishable from those of human follicle stimulating hormone. Recombinant FSH production occurs in genetically modified Chinese Hamster Ovary (CHO) cells cultured in bioreactors. Purification by immunochromatography using an antibody specifically binding FSH results in a highly purified preparation with a consistent FSH isoform profile, and a high specific activity. The biological activity of follitropin alfa is determined by measuring the increase in ovary weight in female rats. The in vivo biological activity of follitropin alfa has been calibrated against the first International Standard for recombinant human follicle stimulating hormone established in 1995 by the Expert Committee on Biological Standards of the World Health Organization. Gonal-f® RFF (follitropin alfa injection) contains no luteinizing hormone (LH) activity. Based on available data derived from physico-chemical tests and bioassays, follitropin alfa and follitropin beta, another recombinant follicle stimulating hormone product, are indistinguishable. | Link | Link | NA |
| 11675 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f RFF Pen | Emd Serono | Emd Serono | Subcutaneous | 300 [iU]/0.5mL | Gonal-f® RFF (follitropin alfa for injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant FSH preparations or one of their excipients. High levels of FSH indicating primary gonadal failure. Uncontrolled thyroid or adrenal dysfunction. Sex hormone dependent tumors of the reproductive tract and accessory organs. An organic intracranial lesion such as a pituitary tumor. Abnormal uterine bleeding of undetermined origin (see "Selection of Patients"). Ovarian cyst or enlargement of undetermined origin (see "Selection of Patients"). Pregnancy. | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11676 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f RFF Pen | Emd Serono | Emd Serono | Subcutaneous | 450 [iU]/0.75mL | Gonal-f® RFF (follitropin alfa for injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant FSH preparations or one of their excipients. High levels of FSH indicating primary gonadal failure. Uncontrolled thyroid or adrenal dysfunction. Sex hormone dependent tumors of the reproductive tract and accessory organs. An organic intracranial lesion such as a pituitary tumor. Abnormal uterine bleeding of undetermined origin (see "Selection of Patients"). Ovarian cyst or enlargement of undetermined origin (see "Selection of Patients"). Pregnancy. | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11677 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f RFF Pen | Emd Serono | Emd Serono | Subcutaneous | 900 [iU]/1.5mL | Gonal-f® RFF (follitropin alfa for injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant FSH preparations or one of their excipients. High levels of FSH indicating primary gonadal failure. Uncontrolled thyroid or adrenal dysfunction. Sex hormone dependent tumors of the reproductive tract and accessory organs. An organic intracranial lesion such as a pituitary tumor. Abnormal uterine bleeding of undetermined origin (see "Selection of Patients"). Ovarian cyst or enlargement of undetermined origin (see "Selection of Patients"). Pregnancy. | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11678 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f RFF Redi-ject | EMD Serono, Inc. | EMD Serono, Inc. | Subcutaneous | 300 [iU]/0.5mL | Gonal-f® RFF (follitropin alfa for injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant FSH preparations or one of their excipients. High levels of FSH indicating primary gonadal failure. Uncontrolled thyroid or adrenal dysfunction. Sex hormone dependent tumors of the reproductive tract and accessory organs. An organic intracranial lesion such as a pituitary tumor. Abnormal uterine bleeding of undetermined origin (see "Selection of Patients"). Ovarian cyst or enlargement of undetermined origin (see "Selection of Patients"). Pregnancy. | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11679 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f RFF Redi-ject | EMD Serono, Inc. | EMD Serono, Inc. | Subcutaneous | 450 [iU]/0.75mL | Gonal-f® RFF (follitropin alfa for injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant FSH preparations or one of their excipients. High levels of FSH indicating primary gonadal failure. Uncontrolled thyroid or adrenal dysfunction. Sex hormone dependent tumors of the reproductive tract and accessory organs. An organic intracranial lesion such as a pituitary tumor. Abnormal uterine bleeding of undetermined origin (see "Selection of Patients"). Ovarian cyst or enlargement of undetermined origin (see "Selection of Patients"). Pregnancy. | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11680 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f RFF Redi-ject | EMD Serono, Inc. | EMD Serono, Inc. | Subcutaneous | 900 [iU]/1.5mL | Gonal-f® RFF (follitropin alfa for injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant FSH preparations or one of their excipients. High levels of FSH indicating primary gonadal failure. Uncontrolled thyroid or adrenal dysfunction. Sex hormone dependent tumors of the reproductive tract and accessory organs. An organic intracranial lesion such as a pituitary tumor. Abnormal uterine bleeding of undetermined origin (see "Selection of Patients"). Ovarian cyst or enlargement of undetermined origin (see "Selection of Patients"). Pregnancy. | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11681 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Gonal-f RFF Redi-ject | EMD Serono, Inc. | EMD Serono, Inc. | Subcutaneous | 150 [iU]/0.25mL | Gonal-f® RFF (follitropin alfa for injection) is contraindicated in women who exhibit: Prior hypersensitivity to recombinant FSH preparations or one of their excipients. High levels of FSH indicating primary gonadal failure. Uncontrolled thyroid or adrenal dysfunction. Sex hormone dependent tumors of the reproductive tract and accessory organs. An organic intracranial lesion such as a pituitary tumor. Abnormal uterine bleeding of undetermined origin (see "Selection of Patients"). Ovarian cyst or enlargement of undetermined origin (see "Selection of Patients"). Pregnancy. | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | GONAL-f is a medicine that contains the active substance follitropin alfa. It is available as a solution for injection in a prefilled pen and as a powder and solvent that are made up into a solution for injection. | GONAL-f is used to treat the following groups: | NA | NA | Link | Link | NA |
| 11682 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Humegon Inj 75 I.U. | Organon Canada Ltd Ltee | Organon Canada Ltd Ltee | Intramuscular | NA | NA | Abdominal or stomach pain (severe) bloating (moderate to severe) chest pain or trouble breathing decreased amount of urine feeling of indigestion general feeling of discomfort or illness headache, severe and throbbing nausea, vomiting, or diarrhea (continuing or severe) pain or swelling in the arms or legs pelvic pain (severe) severe cramping of the uterus shortness of breath or wheezing swelling of the lower legs weight gain (rapid) | NA | NA | NA | NA | Link | Link | NA |
| 11683 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Menopur | Ferring Pharmaceuticals Inc. | Ferring Pharmaceuticals Inc. | Subcutaneous | NA | MENOPUR® is contraindicated in women who exhibit: Prior hypersensitivity to MENOPUR® or menotropins products or one of their excipients High levels of FSH indicating primary ovarian failure [see INDICATIONS AND USAGE] Pregnancy MENOPUR® may cause fetal harm when administered to a pregnant woman [see Use in Specific Populations]. MENOPUR® is contraindicated in women who are pregnant. If this drug is used during pregnancy, or if the woman becomes pregnant while taking this drug, the woman should be apprised of the potential hazard to a fetus. Presence of uncontrolled non-gonadal endocrinopathies (e.g., thyroid, adrenal, or pituitary disorders) [see INDICATIONS AND USAGE] Sex hormone dependent tumors of the reproductive tract and accessory organs Tumors of pituitary gland or hypothalamus Abnormal uterine bleeding of undetermined origin Ovarian cyst or enlargement of undetermined origin, not due to polycystic ovary syndrome | headache, drowsiness, stomach or abdominal pain, bloating, injection site reactions (pain, swelling, irritation, redness), breast enlargement or tenderness, dizziness, nausea, vomiting, diarrhea, shortness of breath, pain/warmth/tenderness centralized in an arm or leg, fever, chills, weakness or aching of muscles or joints, or rash. | Menotropins injection is used to treat infertility in women. Menotropins are a mixture of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) that are produced in the body by the pituitary gland. Menotropins injection is used in women with healthy ovaries who are enrolled in a fertility program... | Menopur is a prescription medicine used to treat the symptoms of Ovulation Induction, Spermatogenesis and Assisted Reproductive Technology. Menopur may be used alone or with other medications. | NA | MENOPUR® is a preparation of gonadotropins (FSH and LH activity), extracted from the urine of postmenopausal women, which has undergone additional steps for purification. | Link | Link | NA |
| 11684 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Ovaleap | Theramex Ireland Limited | Theramex Ireland Limited | Subcutaneous | 300 IU/0.5mL | NA | The most common side effects with Ovaleap (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. For the full list of all side effects reported with Ovaleap, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11685 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Ovaleap | Theramex Ireland Limited | Theramex Ireland Limited | Subcutaneous | 450 IU/0.75mL | NA | The most common side effects with Ovaleap (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. For the full list of all side effects reported with Ovaleap, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11686 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Ovaleap | Theramex Ireland Limited | Theramex Ireland Limited | Subcutaneous | 900 IU/1.5mL | NA | The most common side effects with Ovaleap (which may affect more than 1 in 10 people) are reactions at the injection site (pain, redness, bruising, swelling or irritation). In women, ovarian cysts (sacs of fluid within the ovaries) and headache are also seen in more than 1 patient in 10. For the full list of all side effects reported with Ovaleap, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11687 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Pergonal 75 I.U. | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular | NA | NA | Back pain breast tenderness feeling of warmth, redness of the face, neck, arms, and occasionally, upper chest menstrual changes muscle aches and pains unusual tiredness or weakness | Menotropins injection is used in women with healthy ovaries who are enrolled in a fertility program called assisted reproductive technology (ART). ART uses procedures such as in vitro fertilization (IVF). Menotropins is used together with human chorionic gonadotropin (hCG) in these procedures. | Menotropins injection is used to treat infertility in women. Menotropins are a mixture of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) that are produced in the body by the pituitary gland. | NA | NA | Link | Link | NA |
| 11688 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Pergoveris | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Subcutaneous | NA | NA | The most common side effects reported with Pergoveris (seen in more than 1 patient in 10) are headache, ovarian cysts and injection site reactions (e.g. pain, itching, redness, bruising, swelling or irritation at the site of injection). Treatment can cause overstimulation of the ovaries (known as ovarian hyperstimulation syndrome, OHSS), which can lead to serious medical problems. Mild or moderate OHSS is common, while severe OHSS is uncommon. Thromboembolism (clots in the blood vessels) may occur very rarely, usually associated with severe OHSS. | Pergoveris is a fertility medicine used in women to stimulate the development of follicles, the structures inside the ovaries that contain an egg. | Pergoveris is available as a solution for injection in a pre-filled pen or as a powder and solvent to be made up into a solution for injection. Pergoveris is injected under the skin once a day until the patient has developed a suitable follicle, as assessed using ultrasound scans and by measuring blood oestrogen levels. This may take up to 5 weeks. The recommended starting dose is 150 International Units (IU) of follitropin alfa and 75 IU of lutropin alfa once a day, but this should be tailored to the patient’s response. Using less than the recommended starting dose may not be sufficient to stimulate development of a follicle. If necessary, the dose of follitropin alfa can be increased by adding it as a separate medicine, with 7 to 14 days between each dose increase. | NA | NA | Link | Link | NA |
| 11689 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Pergoveris | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Subcutaneous | NA | NA | The most common side effects reported with Pergoveris (seen in more than 1 patient in 10) are headache, ovarian cysts and injection site reactions (e.g. pain, itching, redness, bruising, swelling or irritation at the site of injection). Treatment can cause overstimulation of the ovaries (known as ovarian hyperstimulation syndrome, OHSS), which can lead to serious medical problems. Mild or moderate OHSS is common, while severe OHSS is uncommon. Thromboembolism (clots in the blood vessels) may occur very rarely, usually associated with severe OHSS. | Pergoveris is a fertility medicine used in women to stimulate the development of follicles, the structures inside the ovaries that contain an egg. | Pergoveris is available as a solution for injection in a pre-filled pen or as a powder and solvent to be made up into a solution for injection. Pergoveris is injected under the skin once a day until the patient has developed a suitable follicle, as assessed using ultrasound scans and by measuring blood oestrogen levels. This may take up to 5 weeks. The recommended starting dose is 150 International Units (IU) of follitropin alfa and 75 IU of lutropin alfa once a day, but this should be tailored to the patient’s response. Using less than the recommended starting dose may not be sufficient to stimulate development of a follicle. If necessary, the dose of follitropin alfa can be increased by adding it as a separate medicine, with 7 to 14 days between each dose increase. | NA | NA | Link | Link | NA |
| 11690 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Pergoveris | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | NA | NA | The most common side effects reported with Pergoveris (seen in more than 1 patient in 10) are headache, ovarian cysts and injection site reactions (e.g. pain, itching, redness, bruising, swelling or irritation at the site of injection). Treatment can cause overstimulation of the ovaries (known as ovarian hyperstimulation syndrome, OHSS), which can lead to serious medical problems. Mild or moderate OHSS is common, while severe OHSS is uncommon. Thromboembolism (clots in the blood vessels) may occur very rarely, usually associated with severe OHSS. | Pergoveris is a fertility medicine used in women to stimulate the development of follicles, the structures inside the ovaries that contain an egg. | Pergoveris is available as a solution for injection in a pre-filled pen or as a powder and solvent to be made up into a solution for injection. Pergoveris is injected under the skin once a day until the patient has developed a suitable follicle, as assessed using ultrasound scans and by measuring blood oestrogen levels. This may take up to 5 weeks. The recommended starting dose is 150 International Units (IU) of follitropin alfa and 75 IU of lutropin alfa once a day, but this should be tailored to the patient’s response. Using less than the recommended starting dose may not be sufficient to stimulate development of a follicle. If necessary, the dose of follitropin alfa can be increased by adding it as a separate medicine, with 7 to 14 days between each dose increase. | NA | NA | Link | Link | NA |
| 11691 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Pergoveris | Merck Europe B.V. | Merck Europe B.V. | Subcutaneous | NA | NA | The most common side effects reported with Pergoveris (seen in more than 1 patient in 10) are headache, ovarian cysts and injection site reactions (e.g. pain, itching, redness, bruising, swelling or irritation at the site of injection). Treatment can cause overstimulation of the ovaries (known as ovarian hyperstimulation syndrome, OHSS), which can lead to serious medical problems. Mild or moderate OHSS is common, while severe OHSS is uncommon. Thromboembolism (clots in the blood vessels) may occur very rarely, usually associated with severe OHSS. | Pergoveris is a fertility medicine used in women to stimulate the development of follicles, the structures inside the ovaries that contain an egg. | Pergoveris is available as a solution for injection in a pre-filled pen or as a powder and solvent to be made up into a solution for injection. Pergoveris is injected under the skin once a day until the patient has developed a suitable follicle, as assessed using ultrasound scans and by measuring blood oestrogen levels. This may take up to 5 weeks. The recommended starting dose is 150 International Units (IU) of follitropin alfa and 75 IU of lutropin alfa once a day, but this should be tailored to the patient’s response. Using less than the recommended starting dose may not be sufficient to stimulate development of a follicle. If necessary, the dose of follitropin alfa can be increased by adding it as a separate medicine, with 7 to 14 days between each dose increase. | NA | NA | Link | Link | NA |
| 11692 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | Merck Ltd. | Merck Ltd. | Intramuscular; Subcutaneous | 50 unit / 0.5 mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11693 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | Merck Ltd. | Merck Ltd. | Intramuscular; Subcutaneous | 100 unit / 0.5 mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11694 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | Organon Canada Inc. | Organon Canada Inc. | Subcutaneous | 833 unit / mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11695 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Intramuscular; Subcutaneous | 50 IU/0.5mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11696 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Intramuscular; Subcutaneous | 75 IU/0.5mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11697 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Intramuscular; Subcutaneous | 100 IU/0.5mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11698 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Intramuscular; Subcutaneous | 150 IU/0.5mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11699 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Intramuscular; Subcutaneous | 200 IU/0.5mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11700 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Intramuscular; Subcutaneous | 225 IU/0.5mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11701 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Subcutaneous | 300 IU/0.36mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11702 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Subcutaneous | 600 IU/0.72mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11703 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Subcutaneous | 150 IU/0.18mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11704 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon | N.V. Organon | N.V. Organon | Subcutaneous | 900 IU/1.08mL | NA | Acid or sour stomach anxiety backache belching bloating chest pain or tightness confusion cough diarrhea difficulty breathing difficulty in speaking dizziness or lightheadedness double vision excess air or gas in the stomach or intestines fainting fast heartbeat fast, weak pulse full feeling headache heartburn inability to move the arms, legs, or facial muscles indigestion loss of appetite noisy breathing passing gas pelvic pain, discomfort, aching, or heaviness rapid weight gain severe nausea slow speech stomach discomfort, upset, or pain, or swelling sudden increase in stomach or shoulder pain sweating trouble breathing unusual or large amount of vaginal bleeding uterine bleeding between menstrual periods vomiting | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11705 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon (600 Iu) | Organon Canada Ltd Ltee | Organon Canada Ltd Ltee | Intramuscular; Subcutaneous | 737 unit / cartridge | NA | The most common side effects reported are a reaction and pain at the injection site. In 4% of the women treated with Puregon in clinical studies, signs and symptoms related to ovarian hyperstimulation syndrome (e.g. feeling sick, weight gain and diarrhoea) have been reported. Ovarian hyperstimulation syndrome occurs when the ovaries over-respond to treatment. | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11706 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon 100 I.U. | Organon Canada Ltd Ltee | Organon Canada Ltd Ltee | Intramuscular; Subcutaneous | NA | NA | The most common side effects reported are a reaction and pain at the injection site. In 4% of the women treated with Puregon in clinical studies, signs and symptoms related to ovarian hyperstimulation syndrome (e.g. feeling sick, weight gain and diarrhoea) have been reported. Ovarian hyperstimulation syndrome occurs when the ovaries over-respond to treatment. | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11707 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Puregon 50 I.U. | Organon Canada Ltd Ltee | Organon Canada Ltd Ltee | Intramuscular; Subcutaneous | NA | NA | The most common side effects reported are a reaction and pain at the injection site. In 4% of the women treated with Puregon in clinical studies, signs and symptoms related to ovarian hyperstimulation syndrome (e.g. feeling sick, weight gain and diarrhoea) have been reported. Ovarian hyperstimulation syndrome occurs when the ovaries over-respond to treatment. | Puregon is a powder and solvent to be made up into a solution for injection. It is also available as a solution for injection in a vial or a cartridge. Puregon contains the active substance follitropin beta. | Puregon is used to treat infertility in women in the following situations: | NA | NA | Link | Link | NA |
| 11708 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Rekovelle | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Subcutaneous | 72 mcg / 2.16 mL | NA | The most common side effects with Rekovelle (which may affect between 1 and 10 people in 100) are headache, discomfort and pain in the pelvic area which may arise from the ovaries, nausea (feeling sick) and tiredness and ovarian hyperstimulation syndrome (OHSS). OHSS is when a woman’s ovaries over-respond to stimulation, causing symptoms such as vomiting, diarrhoea and pain. In severe cases OHSS may lead to difficulty breathing and problems with blood clotting. The frequency of side effects may decrease with repeated treatment cycles. For the full list of all side effects reported with Rekovelle, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11709 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Rekovelle | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Subcutaneous | 36 mcg / 1.08 mL | NA | The most common side effects with Rekovelle (which may affect between 1 and 10 people in 100) are headache, discomfort and pain in the pelvic area which may arise from the ovaries, nausea (feeling sick) and tiredness and ovarian hyperstimulation syndrome (OHSS). OHSS is when a woman’s ovaries over-respond to stimulation, causing symptoms such as vomiting, diarrhoea and pain. In severe cases OHSS may lead to difficulty breathing and problems with blood clotting. The frequency of side effects may decrease with repeated treatment cycles. For the full list of all side effects reported with Rekovelle, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11710 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Rekovelle | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Subcutaneous | 12 mcg / 0.36 mL | NA | The most common side effects with Rekovelle (which may affect between 1 and 10 people in 100) are headache, discomfort and pain in the pelvic area which may arise from the ovaries, nausea (feeling sick) and tiredness and ovarian hyperstimulation syndrome (OHSS). OHSS is when a woman’s ovaries over-respond to stimulation, causing symptoms such as vomiting, diarrhoea and pain. In severe cases OHSS may lead to difficulty breathing and problems with blood clotting. The frequency of side effects may decrease with repeated treatment cycles. For the full list of all side effects reported with Rekovelle, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11711 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Rekovelle | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Subcutaneous | 12 mcg /0.36ml | NA | The most common side effects with Rekovelle (which may affect between 1 and 10 people in 100) are headache, discomfort and pain in the pelvic area which may arise from the ovaries, nausea (feeling sick) and tiredness and ovarian hyperstimulation syndrome (OHSS). OHSS is when a woman’s ovaries over-respond to stimulation, causing symptoms such as vomiting, diarrhoea and pain. In severe cases OHSS may lead to difficulty breathing and problems with blood clotting. The frequency of side effects may decrease with repeated treatment cycles. For the full list of all side effects reported with Rekovelle, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11712 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Rekovelle | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Subcutaneous | 36 mcg /1.08ml | NA | The most common side effects with Rekovelle (which may affect between 1 and 10 people in 100) are headache, discomfort and pain in the pelvic area which may arise from the ovaries, nausea (feeling sick) and tiredness and ovarian hyperstimulation syndrome (OHSS). OHSS is when a woman’s ovaries over-respond to stimulation, causing symptoms such as vomiting, diarrhoea and pain. In severe cases OHSS may lead to difficulty breathing and problems with blood clotting. The frequency of side effects may decrease with repeated treatment cycles. For the full list of all side effects reported with Rekovelle, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11713 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Rekovelle | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Subcutaneous | 72 mcg /2.16ml | NA | The most common side effects with Rekovelle (which may affect between 1 and 10 people in 100) are headache, discomfort and pain in the pelvic area which may arise from the ovaries, nausea (feeling sick) and tiredness and ovarian hyperstimulation syndrome (OHSS). OHSS is when a woman’s ovaries over-respond to stimulation, causing symptoms such as vomiting, diarrhoea and pain. In severe cases OHSS may lead to difficulty breathing and problems with blood clotting. The frequency of side effects may decrease with repeated treatment cycles. For the full list of all side effects reported with Rekovelle, see the package leaflet. | NA | NA | NA | NA | Link | Link | NA |
| 11714 | Th1252 | Follitropin | >Th1252_Follitropin APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 22672.9 | C975H1513N267O304S26 | 7.5 | -0.33 | 55 °C | Circulation half life of 3-4 hours, elimination half life of 35-40 hours | Follitropin is a human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which consists of two non-covalently linked, non-identical glycoproteins designated as the alpha- and beta- subunits. The alpha- and beta- subunits have 92 and 111 amino acids. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin is important in the development of follicles produced by the ovaries. Given by subcutaneous injection, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH. | In women having been diagnosed with primary ovarian failure, it is used in combination with human chorionic gonadotropin (hCG) to assist in ovulation and fertility. In men with hypogonadotrophic hypogonadism, it is used to induce spermatogenesis. Follitropin may also be used to cause the ovary to produce several follicles, which can then be harvested for use in gamete intrafallopian transfer (GIFT) or in vitro fertilization (IVF). | Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development. | Follitropin is a recombinant form of endogenous follicle stimulating hormone (FSH). FSH binds to the follicle stimulating hormone receptor which is a G-coupled transmembrane receptor. Binding of the FSH to its receptor seems to induce phosphorylation and activation of the PI3K (Phosphatidylinositol-3-kinase) and Akt signaling pathway, which is known to regulate many other metabolic and related survival/maturation functions in cells. | Headaches, ovarian cysts, nausea and upper respiratory tract infections occurred in more than 10% of women in clinical trials. In men, the most serious adverse events reported were testicular surgery for cryptorchidism which existed prestudy, hemoptysis, an infected pilonidal cyst, and lymphadenopathy associated with an Epstein-Barr viral infection. Other concerns include overstimulation of the ovaries, pulmonary and vascular complications and multiple births. Post-marketing reports revealed hypersensitivity reactions including anaphylactoid reactions and asthma. Follitropin is contraindicated in pregnant women. No studies have been done in nursing mothers. | NA | The absorption rate is the main driving force behind the pharmokinetics of Follitropin alpha as the rate of absorption was found to be slower than the elimination rate after administration subcutaneously and intramuscularly. The bioavailability is approximately 66-76%. The time to peak after subcutaneous injection in healthy volunteers was 8-16 hours in females and 11-20 hours in males. | * 8 L [female subjects following intravenous administration of a 300 IU dose] | * 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU] * 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU] | NA | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Repronex | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Intramuscular; Subcutaneous | NA | Repronex® (menotropins for injection) is contraindicated in women who have: A high FSH level indicating primary ovarian failure. Uncontrolled thyroid and adrenal dysfunction. An organic intracranial lesion such as a pituitary tumor. The presence of any cause of infertility other than anovulation unless they are candidates for in vitro-fertilization. Abnormal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome. Prior hypersensitivity to menotropins. Repronex® (menotropins for injection) is not indicated in women who are pregnant. There are limited human data on the effects of menotropins when administered during pregnancy. | headache mild stomach pain bloating injection site reactions (redness, pain, swelling, or irritation) breast tenderness or enlargement dizziness ovarian enlargement (abdominal or pelvic pain, tenderness, pressure, or swelling) nausea vomiting diarrhea shortness of breath pain/warmth/tenderness centralized in an arm or leg fever chills drowsiness weakness or aching of muscles or joints, or rash | Menotropins injection is used to treat infertility in women. Menotropins are a mixture of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) that are produced in the body by the pituitary gland. Menotropins injection is used in women with healthy ovaries who are enrolled in a fertility program... | Repronex is a prescription medicine used to treat the symptoms of Ovulation Induction, Assisted Reproductive Technology (ART), and Spermatogenesis. Repronex may be used alone or with other medications. | NA | FOR SUBCUTANEOUS INJECTION AND INTRAMUSCULAR INJECTION | Link | Link | NA |
| 12036 | Th1280 | CR002 | >Th1280_CR002 MVRHPYSVQTQLSTEAKAIWRSMQQQETNLLANLTTNDARDNSKDFQNSKVGAAATSRDEGCNCPIIGEIVISCYWLFEIPPLISE | NA | NA | NA | NA | NA | NA | CR002 is a novel investigational fully human monoclonal antibody that blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. This is a novel therapeutic approach to treat kidney inflammation. | Investigated for use/treatment in nephropathy. | NA | CR002 blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. Diabetic nephropathy, IgA nephropathy, and lupus nephritis are histologically characterized by glomerular mesangial cell proliferation and extracellular matrix accumulation. PDGF-D and its receptors play an important role in the pathogenesis of nephritis, based on their potent induction of mesangial cell proliferation and extracellular matrix accumulation shown both in vitro and in vivo. A fully human monoclonal antibody that neutralizes PDGF-D represents a novel therapeutic approach to block nephritides. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins | NA | NA | NA | NA | Platelet-derived growth factor D | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12037 | Th1280 | CR002 | >Th1280_CR002 MVRHPYSVQTQLSTEAKAIWRSMQQQETNLLANLTTNDARDNSKDFQNSKVGAAATSRDEGCNCPIIGEIVISCYWLFEIPPLISE | NA | NA | NA | NA | NA | NA | CR002 is a novel investigational fully human monoclonal antibody that blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. This is a novel therapeutic approach to treat kidney inflammation. | Investigated for use/treatment in nephropathy. | NA | CR002 blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. Diabetic nephropathy, IgA nephropathy, and lupus nephritis are histologically characterized by glomerular mesangial cell proliferation and extracellular matrix accumulation. PDGF-D and its receptors play an important role in the pathogenesis of nephritis, based on their potent induction of mesangial cell proliferation and extracellular matrix accumulation shown both in vitro and in vivo. A fully human monoclonal antibody that neutralizes PDGF-D represents a novel therapeutic approach to block nephritides. | NA | NA | NA | NA | NA | Antibodies | NA | NA | NA | NA | Platelet-derived growth factor D | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12038 | Th1280 | CR002 | >Th1280_CR002 MVRHPYSVQTQLSTEAKAIWRSMQQQETNLLANLTTNDARDNSKDFQNSKVGAAATSRDEGCNCPIIGEIVISCYWLFEIPPLISE | NA | NA | NA | NA | NA | NA | CR002 is a novel investigational fully human monoclonal antibody that blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. This is a novel therapeutic approach to treat kidney inflammation. | Investigated for use/treatment in nephropathy. | NA | CR002 blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. Diabetic nephropathy, IgA nephropathy, and lupus nephritis are histologically characterized by glomerular mesangial cell proliferation and extracellular matrix accumulation. PDGF-D and its receptors play an important role in the pathogenesis of nephritis, based on their potent induction of mesangial cell proliferation and extracellular matrix accumulation shown both in vitro and in vivo. A fully human monoclonal antibody that neutralizes PDGF-D represents a novel therapeutic approach to block nephritides. | NA | NA | NA | NA | NA | Blood Proteins | NA | NA | NA | NA | Platelet-derived growth factor D | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12039 | Th1280 | CR002 | >Th1280_CR002 MVRHPYSVQTQLSTEAKAIWRSMQQQETNLLANLTTNDARDNSKDFQNSKVGAAATSRDEGCNCPIIGEIVISCYWLFEIPPLISE | NA | NA | NA | NA | NA | NA | CR002 is a novel investigational fully human monoclonal antibody that blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. This is a novel therapeutic approach to treat kidney inflammation. | Investigated for use/treatment in nephropathy. | NA | CR002 blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. Diabetic nephropathy, IgA nephropathy, and lupus nephritis are histologically characterized by glomerular mesangial cell proliferation and extracellular matrix accumulation. PDGF-D and its receptors play an important role in the pathogenesis of nephritis, based on their potent induction of mesangial cell proliferation and extracellular matrix accumulation shown both in vitro and in vivo. A fully human monoclonal antibody that neutralizes PDGF-D represents a novel therapeutic approach to block nephritides. | NA | NA | NA | NA | NA | Globulins | NA | NA | NA | NA | Platelet-derived growth factor D | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12040 | Th1280 | CR002 | >Th1280_CR002 MVRHPYSVQTQLSTEAKAIWRSMQQQETNLLANLTTNDARDNSKDFQNSKVGAAATSRDEGCNCPIIGEIVISCYWLFEIPPLISE | NA | NA | NA | NA | NA | NA | CR002 is a novel investigational fully human monoclonal antibody that blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. This is a novel therapeutic approach to treat kidney inflammation. | Investigated for use/treatment in nephropathy. | NA | CR002 blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. Diabetic nephropathy, IgA nephropathy, and lupus nephritis are histologically characterized by glomerular mesangial cell proliferation and extracellular matrix accumulation. PDGF-D and its receptors play an important role in the pathogenesis of nephritis, based on their potent induction of mesangial cell proliferation and extracellular matrix accumulation shown both in vitro and in vivo. A fully human monoclonal antibody that neutralizes PDGF-D represents a novel therapeutic approach to block nephritides. | NA | NA | NA | NA | NA | Immunoglobulins | NA | NA | NA | NA | Platelet-derived growth factor D | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12041 | Th1280 | CR002 | >Th1280_CR002 MVRHPYSVQTQLSTEAKAIWRSMQQQETNLLANLTTNDARDNSKDFQNSKVGAAATSRDEGCNCPIIGEIVISCYWLFEIPPLISE | NA | NA | NA | NA | NA | NA | CR002 is a novel investigational fully human monoclonal antibody that blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. This is a novel therapeutic approach to treat kidney inflammation. | Investigated for use/treatment in nephropathy. | NA | CR002 blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. Diabetic nephropathy, IgA nephropathy, and lupus nephritis are histologically characterized by glomerular mesangial cell proliferation and extracellular matrix accumulation. PDGF-D and its receptors play an important role in the pathogenesis of nephritis, based on their potent induction of mesangial cell proliferation and extracellular matrix accumulation shown both in vitro and in vivo. A fully human monoclonal antibody that neutralizes PDGF-D represents a novel therapeutic approach to block nephritides. | NA | NA | NA | NA | NA | Immunoproteins | NA | NA | NA | NA | Platelet-derived growth factor D | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12042 | Th1280 | CR002 | >Th1280_CR002 MVRHPYSVQTQLSTEAKAIWRSMQQQETNLLANLTTNDARDNSKDFQNSKVGAAATSRDEGCNCPIIGEIVISCYWLFEIPPLISE | NA | NA | NA | NA | NA | NA | CR002 is a novel investigational fully human monoclonal antibody that blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. This is a novel therapeutic approach to treat kidney inflammation. | Investigated for use/treatment in nephropathy. | NA | CR002 blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. Diabetic nephropathy, IgA nephropathy, and lupus nephritis are histologically characterized by glomerular mesangial cell proliferation and extracellular matrix accumulation. PDGF-D and its receptors play an important role in the pathogenesis of nephritis, based on their potent induction of mesangial cell proliferation and extracellular matrix accumulation shown both in vitro and in vivo. A fully human monoclonal antibody that neutralizes PDGF-D represents a novel therapeutic approach to block nephritides. | NA | NA | NA | NA | NA | Proteins | NA | NA | NA | NA | Platelet-derived growth factor D | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12043 | Th1280 | CR002 | >Th1280_CR002 MVRHPYSVQTQLSTEAKAIWRSMQQQETNLLANLTTNDARDNSKDFQNSKVGAAATSRDEGCNCPIIGEIVISCYWLFEIPPLISE | NA | NA | NA | NA | NA | NA | CR002 is a novel investigational fully human monoclonal antibody that blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. This is a novel therapeutic approach to treat kidney inflammation. | Investigated for use/treatment in nephropathy. | NA | CR002 blocks the activity of excess platelet-derived growth factor-D (PDGF-D), a target shown to play a role in kidney inflammation. Diabetic nephropathy, IgA nephropathy, and lupus nephritis are histologically characterized by glomerular mesangial cell proliferation and extracellular matrix accumulation. PDGF-D and its receptors play an important role in the pathogenesis of nephritis, based on their potent induction of mesangial cell proliferation and extracellular matrix accumulation shown both in vitro and in vivo. A fully human monoclonal antibody that neutralizes PDGF-D represents a novel therapeutic approach to block nephritides. | NA | NA | NA | NA | NA | Serum Globulins | NA | NA | NA | NA | Platelet-derived growth factor D | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12091 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Adjuvants, Immunologic | 5981589 | 09-11-1999 | 24-05-2014 | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Copaxone | TEVA Canada Limited | TEVA Canada Limited | Subcutaneous | 20 mg / mL | COPAXONE is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions (e.g., pain, redness, soreness, itching, swelling, or a hard lump), nausea, vomiting, chills, joint aches, body aches, neck pain, back pain, double vision, headache, increased urge to urinate, weakness, runny nose, swelling in your hands or feet, vaginal itching or discharge, fever, chills, flu symptoms, sore throat, or white patches or sores inside your mouth or on your lips. | Copaxone is a combination of four amino acids (proteins) that affect the immune system. Copaxone injection is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Copaxone will not... | Copaxone is a prescription medicine used to treat the symptoms of Multiple Sclerosis. Copaxone may be used alone or with other medications. | NA | Glatiramer acetate, the active ingredient of COPAXONE, consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000 – 9,000 daltons. Glatiramer acetate is identified by specific antibodies. | Link | Link | NA |
| 12092 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Amino Acids, Peptides, and Proteins | 2191088 | 28-09-2004 | 23-05-2015 | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Copaxone | TEVA Canada Limited | TEVA Canada Limited | Subcutaneous | 40 mg / mL | COPAXONE is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions (e.g., pain, redness, soreness, itching, swelling, or a hard lump), nausea, vomiting, chills, joint aches, body aches, neck pain, back pain, double vision, headache, increased urge to urinate, weakness, runny nose, swelling in your hands or feet, vaginal itching or discharge, fever, chills, flu symptoms, sore throat, or white patches or sores inside your mouth or on your lips. | Copaxone is a combination of four amino acids (proteins) that affect the immune system. Copaxone injection is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Copaxone will not... | Copaxone is a prescription medicine used to treat the symptoms of Multiple Sclerosis. Copaxone may be used alone or with other medications. | NA | Glatiramer acetate, the active ingredient of COPAXONE, consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000 – 9,000 daltons. Glatiramer acetate is identified by specific antibodies. | Link | Link | NA |
| 12093 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Antineoplastic and Immunomodulating Agents | 8232250 | 31-07-2012 | 19-08-2030 | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Copaxone | Sanofi Aventis | Sanofi Aventis | Subcutaneous | 20 mg/1mL | COPAXONE is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions (e.g., pain, redness, soreness, itching, swelling, or a hard lump), nausea, vomiting, chills, joint aches, body aches, neck pain, back pain, double vision, headache, increased urge to urinate, weakness, runny nose, swelling in your hands or feet, vaginal itching or discharge, fever, chills, flu symptoms, sore throat, or white patches or sores inside your mouth or on your lips. | Copaxone is a combination of four amino acids (proteins) that affect the immune system. Copaxone injection is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Copaxone will not... | Copaxone is a prescription medicine used to treat the symptoms of Multiple Sclerosis. Copaxone may be used alone or with other medications. | NA | Glatiramer acetate, the active ingredient of COPAXONE, consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000 – 9,000 daltons. Glatiramer acetate is identified by specific antibodies. | Link | Link | NA |
| 12094 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Antirheumatic Agents | 8399413 | 19-03-2013 | 19-08-2030 | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Copaxone | Teva Neuroscience, Inc. | Teva Neuroscience, Inc. | Subcutaneous | 20 mg/1mL | COPAXONE is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions (e.g., pain, redness, soreness, itching, swelling, or a hard lump), nausea, vomiting, chills, joint aches, body aches, neck pain, back pain, double vision, headache, increased urge to urinate, weakness, runny nose, swelling in your hands or feet, vaginal itching or discharge, fever, chills, flu symptoms, sore throat, or white patches or sores inside your mouth or on your lips. | Copaxone is a combination of four amino acids (proteins) that affect the immune system. Copaxone injection is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Copaxone will not... | Copaxone is a prescription medicine used to treat the symptoms of Multiple Sclerosis. Copaxone may be used alone or with other medications. | NA | Glatiramer acetate, the active ingredient of COPAXONE, consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000 – 9,000 daltons. Glatiramer acetate is identified by specific antibodies. | Link | Link | NA |
| 12095 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Immunologic Factors | 8969302 | 03-03-2015 | 19-08-2030 | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Copaxone | Teva Neuroscience, Inc. | Teva Neuroscience, Inc. | Subcutaneous | 40 mg/1mL | COPAXONE is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions (e.g., pain, redness, soreness, itching, swelling, or a hard lump), nausea, vomiting, chills, joint aches, body aches, neck pain, back pain, double vision, headache, increased urge to urinate, weakness, runny nose, swelling in your hands or feet, vaginal itching or discharge, fever, chills, flu symptoms, sore throat, or white patches or sores inside your mouth or on your lips. | Copaxone is a combination of four amino acids (proteins) that affect the immune system. Copaxone injection is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Copaxone will not... | Copaxone is a prescription medicine used to treat the symptoms of Multiple Sclerosis. Copaxone may be used alone or with other medications. | NA | Glatiramer acetate, the active ingredient of COPAXONE, consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000 – 9,000 daltons. Glatiramer acetate is identified by specific antibodies. | Link | Link | NA |
| 12096 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Immunomodulatory Agents | 9155776 | 13-10-2015 | 19-08-2030 | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Copaxone | Teva Pharmaceutical Industries | Teva Pharmaceutical Industries | Subcutaneous | 20 mg / vial | COPAXONE is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions (e.g., pain, redness, soreness, itching, swelling, or a hard lump), nausea, vomiting, chills, joint aches, body aches, neck pain, back pain, double vision, headache, increased urge to urinate, weakness, runny nose, swelling in your hands or feet, vaginal itching or discharge, fever, chills, flu symptoms, sore throat, or white patches or sores inside your mouth or on your lips. | Copaxone is a combination of four amino acids (proteins) that affect the immune system. Copaxone injection is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Copaxone will not... | Copaxone is a prescription medicine used to treat the symptoms of Multiple Sclerosis. Copaxone may be used alone or with other medications. | NA | Glatiramer acetate, the active ingredient of COPAXONE, consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000 – 9,000 daltons. Glatiramer acetate is identified by specific antibodies. | Link | Link | NA |
| 12097 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Immunosuppressive Agents | 9402874 | 02-08-2016 | 19-08-2030 | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Glatect | Pharmascience Inc | Pharmascience Inc | Subcutaneous | 20 mg / mL | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12098 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Membrane Proteins | NA | NA | NA | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Glatiramer Acetate | Mylan Pharmaceuticals Inc. | Mylan Pharmaceuticals Inc. | Subcutaneous | 40 mg/1mL | NA | feeling short of breath; flushing (sudden warmth, redness, or tingly feeling); rash; or redness, pain, itching, swelling, or a lump where the injection was given. | Glatiramer is injected under the skin. A healthcare provider may teach you how to properly use the medication by yourself. Glatiramer injections are given either daily or 3 times per week, depending on your dose. | Glatiramer is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). | NA | NA | Link | Link | NA |
| 12099 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Peptides | NA | NA | NA | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Glatiramer Acetate | Mylan Pharmaceuticals Inc. | Mylan Pharmaceuticals Inc. | Subcutaneous | 20 mg/1mL | NA | feeling short of breath; flushing (sudden warmth, redness, or tingly feeling); rash; or redness, pain, itching, swelling, or a lump where the injection was given. | Glatiramer is injected under the skin. A healthcare provider may teach you how to properly use the medication by yourself. Glatiramer injections are given either daily or 3 times per week, depending on your dose. | Glatiramer is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). | NA | NA | Link | Link | NA |
| 12100 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Proteins | NA | NA | NA | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Glatopa | Sandoz Inc | Sandoz Inc | Subcutaneous | 20 mg/1mL | Glatopa is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions, skin redness, rash, hives, lightheadedness, flushing, palpitations, anxiety, indigestion, throat constriction, and chest pain | Glatopa is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Glatopa will not cure MS, but it can make relapses occur less often. Glatopa may also be used for purposes not listed... | Glatopa is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. | NA | NA | Link | Link | NA |
| 12101 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | T-Lymphocytes, Helper-Inducer, immunology | NA | NA | NA | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Glatopa | Sandoz Inc | Sandoz Inc | Subcutaneous | 40 mg/1mL | Glatopa is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions, skin redness, rash, hives, lightheadedness, flushing, palpitations, anxiety, indigestion, throat constriction, and chest pain | Glatopa is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Glatopa will not cure MS, but it can make relapses occur less often. Glatopa may also be used for purposes not listed... | Glatopa is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. | NA | NA | Link | Link | NA |
| 12102 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | Vesicular Transport Proteins | NA | NA | NA | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Glatopa | bryant ranch prepack | bryant ranch prepack | Subcutaneous | 40 mg/1mL | Glatopa is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions, skin redness, rash, hives, lightheadedness, flushing, palpitations, anxiety, indigestion, throat constriction, and chest pain | Glatopa is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Glatopa will not cure MS, but it can make relapses occur less often. Glatopa may also be used for purposes not listed... | Glatopa is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. | NA | NA | Link | Link | NA |
| 12103 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | NA | NA | NA | NA | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Glatopa | bryant ranch prepack | bryant ranch prepack | Subcutaneous | 20 mg/1mL | Glatopa is contraindicated in patients with known hypersensitivity to glatiramer acetate or mannitol. | injection site reactions, skin redness, rash, hives, lightheadedness, flushing, palpitations, anxiety, indigestion, throat constriction, and chest pain | Glatopa is used to treat relapsing forms of multiple sclerosis in adults (including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease). Glatopa will not cure MS, but it can make relapses occur less often. Glatopa may also be used for purposes not listed... | Glatopa is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. | NA | NA | Link | Link | NA |
| 12104 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | NA | NA | NA | NA | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Teva-glatiramer Acetate | TEVA Canada Limited | TEVA Canada Limited | Subcutaneous | 40 mg / mL | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12105 | Th1285 | Glatiramer | >Th1285_Glatiramer EAYKAAEKAYAAKEAAKEAAKAKAEKKAAYAKAKAAKYEKKAKKAAAEYKKK | 7000 | C254H422N70O72 | NA | NA | NA | NA | Glatiramer acetate consists of the acetate salts of synthetic polypeptides, containing four naturally occurring amino acids: L-glutamic acid, L-alanine, L-tyrosine, and L-lysine with an average molar fraction of 0.141, 0.427, 0.095, and 0.338, respectively. The average molecular weight of glatiramer acetate is 5,000-9,000 daltons. It is an immunomodulator, licensed in much of the world for reduced frequency of relapses in relapsing-remitting multiple sclerosis. | For reduction of the frequency of relapses in patients with Relapsing-Remitting Multiple Sclerosis. | Glatiramer acetate was originally designed to mimic a protein in myelin, called myelin basic protein, with the intention of inducing EAE (an animal model of MS). Quite to the contrary, it was found to suppress the disease and as a result came to be trialed in human MS. There is some evidence that Glatiramer acetate converts the body's immune response from a Th1 type to a Th2 one, promotes suppressor T cells or acts as an altered peptide ligand. Studies in animals and in vitro systems suggest that upon its administration, glatiramer acetate-specific suppressor T-cells are induced and activated in the periphery. Some fraction of the injected material, either intact or partially hydrolyzed, is presumed to enter the lymphatic circulation, enabling it to reach regional lymph nodes, and some may enter the systemic circulation intact. | Glatiramer acetate (GA) exhibits strong and promiscuous binding to MHC molecules (HLA DRB1* variants) and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression. Furthermore, the GA-specific cells in the brain express the anti-inflammatory cytokines IL-10 and transforming growth factor beta, in addition to brain-derived neurotrophic factor, whereas they do not express the inflammatory cytokine IFN-gamma. Recent evidence also suggests that Glatiramer acetate directly inhibits dendritic cells and monocytes - both of which are circulating antigen presenting cells. | Adverse reactions include injection site reactions, vasodilatation, chest pain, asthenia, infection, pain, nausea, arthralgia, anxiety, and hypertonia. | Hydrolyzed by proteases | NA | NA | NA | NA | NA | NA | NA | NA | HLA class II histocompatibility antigen, DRB1-1 beta chain | Teva-glatiramer Acetate | TEVA Canada Limited | TEVA Canada Limited | Subcutaneous | 20 mg / mL | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12136 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Amino Acids, Peptides, and Proteins | NA | NA | NA | NA | Plasma kallikrein | Kalbitor | Takeda Pharmaceuticals America, Inc. | Takeda Pharmaceuticals America, Inc. | Subcutaneous | 10 mg/1mL | Do not administer KALBITOR to a patient who has known clinical hypersensitivity to KALBITOR. [see WARNINGS AND PRECAUTIONS]. | injection site reactions (bruising, itching, redness, swelling of the skin, pain, rash, or irritation) nausea vomiting stomach pain fever stuffy nose headache diarrhea tired feeling, or sore throat | Kalbitor is used to treat attacks of hereditary angioedema (an immune system disorder). This medicine is for use in adults and children at least 12 years old. Kalbitor is not a cure for hereditary angioedema. Kalbitor may also be used for other purposes not listed in this medication guide. Warnings You... | KALBITOR® (ecallantide) is indicated for treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older. | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | Link | NA |
| 12137 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Analgesics | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12138 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Analgesics, Non-Narcotic | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12139 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Anti-Inflammatory Agents | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12140 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Antirheumatic Agents | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12141 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Blood and Blood Forming Organs | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12142 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Central Nervous System Agents | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12143 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Drugs Used in Hereditary Angioedema | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12144 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Kallikrein Inhibitors | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12145 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Kallikreins, antagonists & inhibitors | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12146 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Peripheral Nervous System Agents | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12147 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Plasma Kallikrein Inhibitor | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12148 | Th1290 | Ecallantide | >Th1290_Ecallantide EAMHSFCAFKADDGPCRAAHPRWFFNIFTRQCEEFIYGGCEGNQNRFESLEECKKMCTRD | 7054 | C305H442N88O91S8 | NA | NA | NA | Following subcutaneous administration of 30 mg ecallantide, the mean elimination half-life was 2.0 ± 0.5 hours [FDA Label]. | Ecallantide is a potent and selective human plasma kallikrein inhibitor that is indicated for the symptomatic treatment of hereditary angioedema. Ecallantide is a recombinant 60-amino-acid protein produced in _Pichia pastoris_ yeast cells that contains three intramolecular disulfide bonds [FDA Label]. It was discovered by phage display technology [A32017]. It shares sequence similarities with the naturally occurring human protein tissue-factor pathway inhibitor (TFPI), which is also known lipoprotein-associated coagulation inhibitor (LACI) [L1458]. The amino acid sequence of two compounds differ by seven amino acids [L1458]. Ecallantide works by blocking kallikrein to participate in the kallikrein-kinin system, which is a complex proteolytic cascade that initiates inflammatory and coagulation pathways [FDA Label]. The protease plasma kallikerin facilitates the conversion of kininogen to bradykinin, which is a pro-inflammatory vasodilator that increases vascular permeability and induces pain [A3362]. Hereditary angioedema is a rare autosomal dominant disorder with mutations to C1-esterase-inhibitor (C1-INH) located on Chromosome 11q, resulting in substantially lower levels of C4 and C1-INH activity [FDA Label]. The disorder is associated with recurrent attacks of severe swelling and is thought to be caused by unregulated activity of kallikrein and excessive bradykinin production [FDA Label]. By reversibly binding to plasma kallikrein, ecallantide displays a rapid on-rate and a slow off-rate that results in high affinity inhibition in the picomolar range [L1458]. Ecallantide is marketed by FDA and EMA under the trade name Kalbitor for subcutaneous injection. Apart from its FDA and EMA indication, ecallantide has been used off label in the management of nonhistaminergic angioedema, not due to HAE [A32017]. | Indicated for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older [FDA Label]. | Intravenous administration of ecallantide doses =20 mg/m^2 resulted in prolongation of activated partial thromboplastin time (aPTT) without an indication of bleeding. Ecallantide administration has been associated with instances of arrhythmia. In a clinical trial of patients experiencing acute attacks of hereditary angioedema (HAE), intravenous administration of ecallantide demonstrated a significant improvement in symptoms affecting the oropharynx, abdomen, gastrointestinal tract, and limbs within 4 hours post-administration compared to placebo [A32016]. A substantial decrease in the severity and duration of attacks was also observed in patients with moderate-to-severe HAE attacks [A32014]. In clinical trials, ecallantide had no significant effect on the QTc interval, heart rate, or any other components of the ECG [FDA Label]. | The kallikrein-kinin system is a complex proteolytic cascade that promotes inflammatory and coagulation pathways. Human plasma kallikrein acts as a protease to mediate the conversion of High Molecular Weight (HMW) kininogen to bradykinin, which is a vasoactive mediator that increases vascular permeability and induces localized swelling, inflammation, and pain [FDA Label]. The actions of kallikrein is regulated by the major endogenous inhibitor, C1-esterase-inhibitor (C1-INH). C1-INH also functions to regulate the activation of the complement and intrinsic coagulation (contact system pathway) [FDA Label], which also initiates the production of bradykinin. Upon audoactivation via exposure to negatively charged surfaces, factor XII promotes the generation of factor XIIa and kallikrein [A32014]. C1-INH inhibits both factor XIIa and kallikrein [A32014]. Kallikrein may in turn reciprocally activate more FXII [A32017]. Hereditary angioedema is associated with a deficiency of the C1 inhibitor is caused by a mutation in the C1 INH gene [A32014]. Resulting effect is excessive production of the vasodilator, bradykinin. The actions of bradykinin produce typical edematous signs and symptoms of hereditary angioedema by enhancing vascular and endothelial permeability, leading to increased outflow of plasma into the interstitium to produce local edema [A32014]. Ecallantide is a potent, specific and reversible plasma kallikrein inhibitor with an Inhibitory Constant (Ki) of 25 pM [A32014]. Upon binding to kallikrein and blocking its active site, ecallantide prevents the conversion of HMW kininogen to bradykinin and attenuates the production of bradykinin [FDA Label]. By blocking the actions of kallikrein, ecallantide also reduces further activation of fXIIa, halting the positive feedback mechanism leading to more kallikrein production [A32017]. | While there have been no reports of overdose with ecallantide, patients with hereditary angioedema have received single doses up to 90 mg intravenously without evidence of dose-related toxicity [FDA Label]. There are no animal or human studies to assess the carcinogenic or mutagenic potential of ecallantide [FDA Label]. In rats receiving subcutaneous doses up to 25 mg/kg/day, there were no observable effects on fertility reproductive performance [FDA Label]. An approximate lethal dose was identified as 25 mg/kg intravenously in rats and 5 mg/kg intravenously in rabbits [L1458]. | Ecallantide does not undergo metabolism mediated by the cytochrome P-450 system [A32017]. No _in vitro_ metabolism studies were performed with ecallantide [FDA Label]. | Following the administration of a single 30 mg subcutaneous dose of ecallantide in healthy subjects, a mean (± standard deviation) peak plasma concentration (Cmax) of 586 ± 106 ng/mL was achieved [FDA Label]. The time to reach Cmax (Tmax) was approximately 2 to 3 hours post-dose [FDA Label]. The mean area under the concentration-time curve (AUC) was 3017 ± 402 ng*hr/mL [FDA Label]. | The volume of distribution was 26.4 ± 7.8 L in healthy individuals [FDA Label]. Intravenous and subcutaneous administration of ecallantide in patients and in healthy subjects resulted in rapid distribution in the vascular compartment [A32014]. | Plasma clearance was 153 ± 20 mL/min following a single subcutaneous dose of 30 mg ecallantide in healthy subjects [FDA Label]. Inter-individual variability in patients and healthy individuals was 38% for clearance [A32014]. | Sensory System Agents | NA | NA | NA | NA | Plasma kallikrein | NA | NA | NA | NA | NA | NA | NA | NA | NA | (2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(1R,2aS,4S,5aS,8aS,11aR,13S,14aS,16S,17aS,19S,20aS,22S,23aS,25S,26aS,28S,29aS,31R,32aS,35aS,36R,38aS,39S,41aS,42S,44aS,45S,48R,50aS,51S,53aS,54S,56aS,57S,59aS,60S,63S,66S,69S,72S,75S,78S,84S,87R,96S,99S)-22,42,45-tris(4-aminobutyl)-31-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-carboxybutanoyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-29a,72,78-tris(2-amino-2-oxoethyl)-14a,75-bis(3-amino-3-oxopropyl)-2a,23a,25,32a,35a,66-hexabenzyl-26a,99-bis[(2S)-butan-2-yl]-17a,41a,59a,69-tetrakis(3-carbamimidamidopropyl)-5a,8a,51,54,63,84-hexakis(2-carboxyethyl)-13,16-bis(carboxymethyl)-20a-[(1S)-1-hydroxyethyl]-60-(hydroxymethyl)-96-[(4-hydroxyphenyl)methyl]-50a-(1H-imidazol-5-ylmethyl)-38a-(1H-indol-3-ylmethyl)-19,28,53a,56a-tetramethyl-57-(2-methylpropyl)-39-(2-methylsulfanylethyl)-1a,3,4a,7a,9,10a,12,13a,15,16a,18,19a,21,22a,24,25a,27,28a,30,31a,34a,37a,38,40a,41,43a,44,47,49a,50,52a,53,55a,56,58a,59,61a,62,65,68,71,74,77,80,83,86,89,92,95,98-pentacontaoxo-33,34,63a,64a,67a,68a-hexathia-a,2,3a,6a,8,9a,11,12a,14,15a,17,18a,20,21a,23,24a,26,27a,29,30a,33a,36a,37,39a,40,42a,43,46,48a,49,51a,52,54a,55,57a,58,60a,61,64,67,70,73,76,79,82,85,88,91,94,97-pentacontazapentacyclo[85.74.4.448,111.04,8.0144,148]nonahexacontahectane-36-carbonyl]amino]-3-hydroxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]butanedioic acid | NA | Link | NA | NA |
| 12449 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Amino Acids, Peptides, and Proteins | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | Natpar | Takeda Pharmaceuticals International Ag Ireland Branch | Takeda Pharmaceuticals International Ag Ireland Branch | Subcutaneous | 25 ?g | NATPARA is contraindicated in patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions (e.g., anaphylaxis, angioedema, and urticaria) have occurred with NATPARA [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS]. | Abdominal or stomach cramps or pain blurred vision confusion constipation convulsions depression difficulty with breathing dizziness dry mouth headache incoherent speech increased urination irregular heartbeats loss of appetite metallic taste muscle cramps in the hands, arms, feet, legs, or face muscle weakness nausea nervousness numbness and tingling around the mouth, fingertips, or feet pounding in the ears slow or fast heartbeat thirst tremor unusual tiredness vomiting weight loss | NA | NA | NA | NA | Link | Link | NA |
| 12450 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Calcium Homeostasis | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | Natpar | Takeda Pharmaceuticals International Ag Ireland Branch | Takeda Pharmaceuticals International Ag Ireland Branch | Subcutaneous | 50 ?g | NATPARA is contraindicated in patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions (e.g., anaphylaxis, angioedema, and urticaria) have occurred with NATPARA [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS]. | Abdominal or stomach cramps or pain blurred vision confusion constipation convulsions depression difficulty with breathing dizziness dry mouth headache incoherent speech increased urination irregular heartbeats loss of appetite metallic taste muscle cramps in the hands, arms, feet, legs, or face muscle weakness nausea nervousness numbness and tingling around the mouth, fingertips, or feet pounding in the ears slow or fast heartbeat thirst tremor unusual tiredness vomiting weight loss | NA | NA | NA | NA | Link | Link | NA |
| 12451 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Calcium-Regulating Hormones and Agents | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | Natpar | Takeda Pharmaceuticals International Ag Ireland Branch | Takeda Pharmaceuticals International Ag Ireland Branch | Subcutaneous | 75 ?g | NATPARA is contraindicated in patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions (e.g., anaphylaxis, angioedema, and urticaria) have occurred with NATPARA [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS]. | Abdominal or stomach cramps or pain blurred vision confusion constipation convulsions depression difficulty with breathing dizziness dry mouth headache incoherent speech increased urination irregular heartbeats loss of appetite metallic taste muscle cramps in the hands, arms, feet, legs, or face muscle weakness nausea nervousness numbness and tingling around the mouth, fingertips, or feet pounding in the ears slow or fast heartbeat thirst tremor unusual tiredness vomiting weight loss | NA | NA | NA | NA | Link | Link | NA |
| 12452 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Hormones | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | Natpar | Takeda Pharmaceuticals International Ag Ireland Branch | Takeda Pharmaceuticals International Ag Ireland Branch | Subcutaneous | 100 ?g | NATPARA is contraindicated in patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions (e.g., anaphylaxis, angioedema, and urticaria) have occurred with NATPARA [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS]. | Abdominal or stomach cramps or pain blurred vision confusion constipation convulsions depression difficulty with breathing dizziness dry mouth headache incoherent speech increased urination irregular heartbeats loss of appetite metallic taste muscle cramps in the hands, arms, feet, legs, or face muscle weakness nausea nervousness numbness and tingling around the mouth, fingertips, or feet pounding in the ears slow or fast heartbeat thirst tremor unusual tiredness vomiting weight loss | NA | NA | NA | NA | Link | Link | NA |
| 12453 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Hormones, Hormone Substitutes, and Hormone Antagonists | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | NATPARA (parathyroid hormone) | Shire-NPS Pharmaceuticals, Inc. | Shire-NPS Pharmaceuticals, Inc. | Subcutaneous | 25 ug/0.08mL | NATPARA is contraindicated in patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions (e.g., anaphylaxis, angioedema, and urticaria) have occurred with NATPARA [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS]. | Abdominal or stomach cramps or pain blurred vision confusion constipation convulsions depression difficulty with breathing dizziness dry mouth headache incoherent speech increased urination irregular heartbeats loss of appetite metallic taste muscle cramps in the hands, arms, feet, legs, or face muscle weakness nausea nervousness numbness and tingling around the mouth, fingertips, or feet pounding in the ears slow or fast heartbeat thirst tremor unusual tiredness vomiting weight loss | NA | NA | NA | NA | Link | Link | NA |
| 12454 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Parathyroid Hormones and Analogues | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | NATPARA (parathyroid hormone) | Shire-NPS Pharmaceuticals, Inc. | Shire-NPS Pharmaceuticals, Inc. | Subcutaneous | 50 ug/0.08mL | NATPARA is contraindicated in patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions (e.g., anaphylaxis, angioedema, and urticaria) have occurred with NATPARA [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS]. | Abdominal or stomach cramps or pain blurred vision confusion constipation convulsions depression difficulty with breathing dizziness dry mouth headache incoherent speech increased urination irregular heartbeats loss of appetite metallic taste muscle cramps in the hands, arms, feet, legs, or face muscle weakness nausea nervousness numbness and tingling around the mouth, fingertips, or feet pounding in the ears slow or fast heartbeat thirst tremor unusual tiredness vomiting weight loss | NA | NA | NA | NA | Link | Link | NA |
| 12455 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Peptide Hormones | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | NATPARA (parathyroid hormone) | Shire-NPS Pharmaceuticals, Inc. | Shire-NPS Pharmaceuticals, Inc. | Subcutaneous | 75 ug/0.08mL | NATPARA is contraindicated in patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions (e.g., anaphylaxis, angioedema, and urticaria) have occurred with NATPARA [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS]. | Abdominal or stomach cramps or pain blurred vision confusion constipation convulsions depression difficulty with breathing dizziness dry mouth headache incoherent speech increased urination irregular heartbeats loss of appetite metallic taste muscle cramps in the hands, arms, feet, legs, or face muscle weakness nausea nervousness numbness and tingling around the mouth, fingertips, or feet pounding in the ears slow or fast heartbeat thirst tremor unusual tiredness vomiting weight loss | NA | NA | NA | NA | Link | Link | NA |
| 12456 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Peptides | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | NATPARA (parathyroid hormone) | Shire-NPS Pharmaceuticals, Inc. | Shire-NPS Pharmaceuticals, Inc. | Subcutaneous | 100 ug/0.08mL | NATPARA is contraindicated in patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions (e.g., anaphylaxis, angioedema, and urticaria) have occurred with NATPARA [see WARNINGS AND PRECAUTIONS, ADVERSE REACTIONS]. | Abdominal or stomach cramps or pain blurred vision confusion constipation convulsions depression difficulty with breathing dizziness dry mouth headache incoherent speech increased urination irregular heartbeats loss of appetite metallic taste muscle cramps in the hands, arms, feet, legs, or face muscle weakness nausea nervousness numbness and tingling around the mouth, fingertips, or feet pounding in the ears slow or fast heartbeat thirst tremor unusual tiredness vomiting weight loss | NA | NA | NA | NA | Link | Link | NA |
| 12457 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | Preotact | Nps Pharma Holdings Limited | Nps Pharma Holdings Limited | Subcutaneous | 100 µg | NA | The most common side effects reported with Pergoveris (seen in more than 1 patient in 10) are headache, ovarian cysts and injection site reactions (e.g. pain, itching, redness, bruising, swelling or irritation at the site of injection). Treatment can cause overstimulation of the ovaries (known as ovarian hyperstimulation syndrome, OHSS), which can lead to serious medical problems. Mild or moderate OHSS is common, while severe OHSS is uncommon. | Preotact is a medicine that contains the active substance parathyroid hormone. It is available as a powder and solvent, contained within a cartridge, to be made up into a solution for injection using a special injection pen. It is also available as a pre-filled pen incorporating the cartridge containing the powder and solvent Each cartridge contains 14 doses. | Preotact is used for the treatment of osteoporosis (a disease that makes bones fragile) in postmenopausal women who are at high risk of fractures. Preotact has been shown to significantly reduce vertebral (spine) fractures, but not hip fractures. | NA | NA | Link | Link | NA |
| 12458 | Th1324 | Parathyroid hormone | >Th1324_Parathyroid_hormone SVSEIQLMHNLGKHLNSMERVEWLRKKLQDVHNFVALGAPLAPRDAGSQRPRKKEDNVLVESHEKSLGEADKADVNVLTKAKSQ | 9420 | C408H674N126O126S2 | NA | NA | NA | 1.5 hours. | Parathyroid hormone (PTH) is a single-chain polypeptide composed of 84 amino acids. Available as Preotact, it is an identical form of human recombinant hormome which produced as a fusion protein undergoeing post-translational processing involving the cleavage of the OmpA leader sequence, leaving the mature protein as a single-chain 84 amino-acids polypeptide (9.4 kDa). Preotact is used in the treatment of osteoporosis in postmenopausal women at high risk of osteoporotic fractures and is marketed in Europe by Nycomed. Preos is a registered trade mark owned by NPS Pharmaceuticals, Inc. The name Preos and the New Drug Application is pending approval by the U.S. Food and Drug Administration (FDA). | For use/treatment in osteoporosis. | Parathyroid hormone is responsible for the fine regulation of serum calcium concentration on a minute-to-minute basis. This is achieved by the acute effects of the hormone on calcium resorption in bone and calcium reabsorption in the kidney. The phosphate mobilized from bone is excreted into the urine by means of the hormone's influence on renal phosphate handling. Parathyroid hormone also stimulates calcium absorption in the intestine, this being mediated indirectly by 1,25-dihydroxyvitamin D. Thus, a hypocalcemic stimulus of parathyroid hormone secretion results in an increased influx of calcium from three sources (bone, kidney, and intestine), resulting in a normalization of the serum calcium concentration without change in the serum phosphate concentration. | The biological actions of rhPTH are mediated through binding to at least two distinct high- affinity cell-surface receptors specific for the N-terminal and C-terminal regions of the molecule, both of which are required for normal bone metabolism. The N-terminal portion of the molecule is primarily responsible for the bone building effects of parathyroid hormone. The C-terminal portion of the molecule has antiresorptive activity and is necessary for normal regulation of N-terminal fragment activity. | NA | PTH is primarily metabolised in the liver with lesser contributions by the kidney. Amino terminal fragments are metabolised in the liver while carboxyl terminal groups travel to the kidney for metabolism where they are also thought to have a role in regulation of PTH. Only about 30% of circulating hormone is present as the unfragmented form. | The absolute bioavailability after subcutaneous administration in the abdomen is 55% for doses of 100 micrograms. | The volume of distribution at steady-state following intravenous administration is approximately 5.4 liters with an interpatient variability of about 40%. | NA | Thyroid Products | NA | NA | NA | NA | Parathyroid hormone/parathyroid hormone-related peptide receptor,Parathyroid hormone 2 receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12503 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12504 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Antibodies | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12505 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Antineoplastic Agents | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12506 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Antineoplastic Agents, Immunological | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12507 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Blood Proteins | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12508 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Globulins | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12509 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Immunoglobulins | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12510 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Immunoproteins | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12511 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Proteins | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12512 | Th1329 | CT-011 | >Th1329_CT-011 MHCLPVLVILLLLIASTPSVDARPKTKDDVPLASFHGADNANRILRTLWNLRGCCEDKTCCFIG | NA | NA | NA | NA | NA | NA | CT-011 is a humanized monoclonal antibody directed against a B7 family-associated protein, in patients with advanced haematological malignancies. It is directed against human PD-1 (programmed cell death 1; PDCD1), with immunomodulating and antitumor activities. | Investigated for use/treatment in cancer/tumors (unspecified). | NA | CT-011 blocks interaction between the receptor PD-1 with its ligands, PD-1 ligand 1 (PD-1L1) and PD-1 ligand 2 (PD-1L2), resulting in the attenuation of apoptotic processes in lymphocytes, primarily effector/memory T cells, and the augmentation of the anti-tumor activities of NK cells. PD-1 is an inhibitory receptor belonging to the B7-receptor family that is expressed on lymphocytes and myeloid cells; its ligands, PD-1L1 and PD-1L2, are expressed not only by hematopoietic cells but also by cells in non-lymphoid tissues. | NA | NA | NA | NA | NA | Serum Globulins | NA | NA | NA | NA | Programmed cell death protein 1 | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12993 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Amino Acids, Peptides, and Proteins | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Elonva | N.V. Organon | N.V. Organon | Subcutaneous | 100 micrograms | NA | In women, the most common side effects with Elonva (which may affect up to 1 in 10 people) are headache, nausea (feeling sick), tiredness, pelvic pain and discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). OHSS occurs when the ovaries over-respond to treatment, causing abdominal swelling and pain, nausea and diarrhoea. | NA | NA | NA | NA | Link | Link | NA |
| 12994 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Drugs that are Mainly Renally Excreted | NA | NA | NA | NA | Follicle-stimulating hormone receptor | Elonva | N.V. Organon | N.V. Organon | Subcutaneous | 150 micrograms | NA | In women, the most common side effects with Elonva (which may affect up to 1 in 10 people) are headache, nausea (feeling sick), tiredness, pelvic pain and discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). OHSS occurs when the ovaries over-respond to treatment, causing abdominal swelling and pain, nausea and diarrhoea. | NA | NA | NA | NA | Link | Link | NA |
| 12995 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Follicle Stimulating Hormone | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12996 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Genito Urinary System and Sex Hormones | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12997 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Gonadotropins | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12998 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Gonadotropins, Pituitary | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 12999 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Hormones | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 13000 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Hormones, Hormone Substitutes, and Hormone Antagonists | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 13001 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Peptide Hormones | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 13002 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Peptides | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 13003 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Pituitary Hormones | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 13004 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Pituitary Hormones, Anterior | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 13005 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Recombinant Proteins | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 13006 | Th1375 | Corifollitropin alfa | >Th1375_Corifollitropin_alfa APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | 25398.0389 | NA | NA | NA | NA | Corifollitropin alfa has a longer half-life compared with FSH and thus requires less frequent dosing [A32516]., Corifollitropin alfa has an elimination half-life of 70 hours (59-82 hours) [L2270]. | Corifollitropin alfa, also known as _Elonva_ is used in women undergoing fertility treatment to stimulate the development of more than one mature egg (oocyte) at a time in the ovaries. This drug used together with _a gonadotropin-releasing hormone (GnRH) antagonist_, a type of medicine also used in fertility treatments. Elonva is available only by prescription [L2270]. In July 2014, Merck announced the receipt of a Complete Response Letter (CRL) from the U.S. FDA for its New Drug Application for this drug. Corifollitropin alfa is marketed as Elonva in more than 75 countries [L2272]. Corifollitropin alfa is produced by a method known as ‘recombinant DNA technology’. This means that it is made by cells into which a DNA has been introduced that makes them able to produce corifollitropin alfa [L2270]. Multiple studies and a meta-analysis suggest that corifollitropin alfa is as efficacious as recombinant FSH in terms of live birth rate, ongoing pregnancy rate, as well as clinical pregnancy rate. The increased in the number of eggs retrieved under corifollitropin alfa regimen represents the elevated effectiveness of this drug, however, warns at the same time against the possibility of an increased risk of ovarian hyperstimulation in the high responder study group of women [L2276], [A32526]. | Controlled ovarian stimulation [L2273] in cases of women who are undergoing fertility treatment to stimulate the development of more than one mature egg simultaneously in the ovaries in combination with a gonadotrophin-releasing hormone (GnRH) antagonist (a type of medicine also used in fertility treatments)[L2270]. | A single dose of corifollitropin alfa could initiate and sustain multi-follicular growth in patients undergoing controlled ovarian stimulation, such as during in vitro fertilization or intracytoplasmic sperm injection [L2274]. This drug is structurally similar to follicle stimulating hormone (FSH), a hormone naturally present in females. FSH stimulates the production of eggs (ova) in the ovaries. In corifollitropin alfa, a peptide is attached to the FSH to prolong its activity. As a result, one single dose of the medicine can be administered to stimulate egg production for seven days, replacing daily injections that are normally needed with other FSH medicines [L2270]. In phase III clinical trials, the number of oocytes retrieved following the administration of corifollitropin alfa was slightly higher compared with the number observed with daily recombinant FSH treatment [L2274]. | Corifollitropin alfa is a long-lasting single injection fusion protein which lacks luteinizing hormone (LH) activity. Only one injection is needed for the first 7 days, which replaces the first 7 daily injections of traditional follicle stimulating hormone (FSH). It is a follicle-stimulation hormone (human a-subunit reduced), a combination of follicle stimulation hormone (human ß-subunit reduced) fusion protein with 118-145-chorionic gonadotropin (human ß-subunit) [L2270]. Frequent, repetitive injections increase stress and error rates, and are often a burden for women, leading to therapy noncompliance [L2277]. The agent comprises an alpha-subunit, which is identical to that of FSH, and a beta-subunit, which is produced by the fusion of the C-terminal peptide from the beta-subunit of chorionic gonadotropin to the beta-subunit of FSH [A32516]. Corifollitropin alfa serves as a sustained follicle stimulant that has similar pharmacological effects to recombinant follicle stimulating hormone (rFSH), however, with a relatively long elimination half-life, resulting in a longer duration of action. This is achieved using site-directed mutagenesis and gene transfer techniques to create a glycoprotein that consists of an a-subunit that is identical to human follicle stimulating hormone (FSH) noncovalently bound to a _ß-subunit_ comprised of a complete _ß-chain_ of human FSH elongated by the carboxyterminal peptide of the ß-subunit of human chorionic gonadotrophin (hCG) [L2271]. This unit interacts with the FSH receptor [A32516] to stimulate the release of oocytes. Corifollitropin alfa does not demonstrate any intrinsic LH/hCG activity [L2270]. | The most common side effects with Elonva (seen in between 1 and 10 patients in 100) include a headache, nausea, fatigue, pelvic pain and/or discomfort, breast tenderness and ovarian hyperstimulation syndrome (OHSS). This syndrome occurs when the ovaries have a heightened response to therapy, leading to abdominal swelling and pain, nausea and diarrhea [L2270]. More than one injection of Elonva within one treatment cycle or an excessively high dose of Elonva and/or (rec)FSH can increase the risk of ovarian hyperstimulation syndrome [L2270], which may cause swollen or painful ovaries, abdominal bloating, nausea, and a weight gain of up to 3kg [L2275]. In severe cases, ovarian hyperstimulation syndrome may cause rapid weight gain ranging from 15 to 20 kilograms in 5-10 days. Severe abdominal pain, severe, persistent nausea, and vomiting, decreased urination, and abdominal bloating, as well as other generalized symptoms, may occur [L2275]. About 1 - 2 % of women undergoing ovarian stimulation develop a severe form of ovarian hyperstimulation syndrome (OHSS). Severe OHSS can be life-threatening. Complications may include: ascites, pulmonary edema, electrolyte disturbances (sodium, potassium, others), thrombosis in large vessels, usually in the lower extremities, renal failure, ovarian torsion, rupture of ovarian cysts. Some of these conditions can lead to hemorrhage, respiratory failure, spontaneous miscarriage or pregnancy termination due to complications, resulting in death [L2270]. | The metabolic fate of corifollitropin alfa highly resembles that of endogenous glycoprotein hormones, which predominantly is comprised of kidney clearance and the urinary excretion of the intact protein in parallel to kidney catabolism [A32519]. | After one single subcutaneous injection of this drug, the maximal serum concentration is 4.24 ng/mL (2.49-7.21 ng/mL1) and is reached 44 hours (35-57 h) post-dose administration. Its absolute bioavailability is 58% (48-70%) [L2270]. | Distribution, metabolism and elimination of corifollitropin alfa are very similar to other gonadotropins, such as FSH, hCG and LH [L2273]. After absorption into the blood, corifollitropin alfa is distributed mainly to the ovaries and the kidneys. The steady-state volume of distribution is 9.2 L [L2273]. Exposure to corifollitropin alfa increases in a linear fashion with the dose within a range of 60 micrograms - 240 micrograms [L2270]. | 0.13 L/h (0.10-0.18 L/h1) [L2270] | Sex Hormones and Modulators of the Genital System | NA | NA | NA | NA | Follicle-stimulating hormone receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 14777 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14778 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Gastrointestinal Agents | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14779 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Hormones | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14780 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Hormones, Hormone Substitutes, and Hormone Antagonists | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14781 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Nerve Tissue Proteins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14782 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Neuropeptides | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14783 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Pancreatic Hormones | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14784 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Peptide Hormones | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14785 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Peptides | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 14786 | Th1537 | Pancreatic Polypeptide | >Th1537_Pancreatic_Polypeptide MAAARLCLSLLLLSTCVALLLQPLLGAQGAPLEPVYPGDNATPEQMAQYAADLRRYINMLTRPRYGKRHKEDTLAFSEWGSPHAAVPRELSPLDL | NA | NA | NA | NA | NA | NA | Pancreatic Polypeptide has been investigated for the treatment of Diabetes Mellitus, Type 1. | NA | NA | NA | NA | NA | NA | NA | NA | Proteins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4S)-5-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-1-[(2S)-2-[[(2S)-1-[[(2S)-1-amino-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]carbamoyl]pyrrolidin-1-yl]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-aminopropanoyl]pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]propanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoic acid | NA | Link | NA | NA |
| 15619 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins | NA | NA | NA | NA | NA | Humegon Inj 75 I.U. | Organon Canada Ltd Ltee | Organon Canada Ltd Ltee | Intramuscular | NA | NA | Abdominal or stomach pain (severe) bloating (moderate to severe) chest pain or trouble breathing decreased amount of urine feeling of indigestion general feeling of discomfort or illness headache, severe and throbbing nausea, vomiting, or diarrhea (continuing or severe) pain or swelling in the arms or legs pelvic pain (severe) severe cramping of the uterus shortness of breath or wheezing swelling of the lower legs weight gain (rapid) | NA | NA | NA | NA | Link | Link | NA |
| 15620 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Gonadotropins | NA | NA | NA | NA | NA | Menopur | Ferring Pharmaceuticals Inc. | Ferring Pharmaceuticals Inc. | Subcutaneous | NA | MENOPUR® is contraindicated in women who exhibit: Prior hypersensitivity to MENOPUR® or menotropins products or one of their excipients High levels of FSH indicating primary ovarian failure [see INDICATIONS AND USAGE] Pregnancy MENOPUR® may cause fetal harm when administered to a pregnant woman [see Use in Specific Populations]. MENOPUR® is contraindicated in women who are pregnant. If this drug is used during pregnancy, or if the woman becomes pregnant while taking this drug, the woman should be apprised of the potential hazard to a fetus. Presence of uncontrolled non-gonadal endocrinopathies (e.g., thyroid, adrenal, or pituitary disorders) [see INDICATIONS AND USAGE] Sex hormone dependent tumors of the reproductive tract and accessory organs Tumors of pituitary gland or hypothalamus Abnormal uterine bleeding of undetermined origin Ovarian cyst or enlargement of undetermined origin, not due to polycystic ovary syndrome | headache, drowsiness, stomach or abdominal pain, bloating, injection site reactions (pain, swelling, irritation, redness), breast enlargement or tenderness, dizziness, nausea, vomiting, diarrhea, shortness of breath, pain/warmth/tenderness centralized in an arm or leg, fever, chills, weakness or aching of muscles or joints, or rash. | Menotropins injection is used to treat infertility in women. Menotropins are a mixture of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) that are produced in the body by the pituitary gland. Menotropins injection is used in women with healthy ovaries who are enrolled in a fertility program... | Menopur is a prescription medicine used to treat the symptoms of Ovulation Induction, Spermatogenesis and Assisted Reproductive Technology. Menopur may be used alone or with other medications. | NA | MENOPUR® is a preparation of gonadotropins (FSH and LH activity), extracted from the urine of postmenopausal women, which has undergone additional steps for purification. | Link | Link | NA |
| 15621 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Gonadotropins, Pituitary | NA | NA | NA | NA | NA | Pergonal 75 I.U. | Emd Serono, A Division Of Emd Inc., Canada | Emd Serono, A Division Of Emd Inc., Canada | Intramuscular | NA | NA | Back pain breast tenderness feeling of warmth, redness of the face, neck, arms, and occasionally, upper chest menstrual changes muscle aches and pains unusual tiredness or weakness | Menotropins injection is used in women with healthy ovaries who are enrolled in a fertility program called assisted reproductive technology (ART). ART uses procedures such as in vitro fertilization (IVF). Menotropins is used together with human chorionic gonadotropin (hCG) in these procedures. | Menotropins injection is used to treat infertility in women. Menotropins are a mixture of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) that are produced in the body by the pituitary gland. | NA | NA | Link | Link | NA |
| 15622 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Hormones | NA | NA | NA | NA | NA | Repronex | Ferring Pharmaceuticals | Ferring Pharmaceuticals | Intramuscular; Subcutaneous | NA | Repronex® (menotropins for injection) is contraindicated in women who have: A high FSH level indicating primary ovarian failure. Uncontrolled thyroid and adrenal dysfunction. An organic intracranial lesion such as a pituitary tumor. The presence of any cause of infertility other than anovulation unless they are candidates for in vitro-fertilization. Abnormal bleeding of undetermined origin. Ovarian cysts or enlargement not due to polycystic ovary syndrome. Prior hypersensitivity to menotropins. Repronex® (menotropins for injection) is not indicated in women who are pregnant. There are limited human data on the effects of menotropins when administered during pregnancy. | headache mild stomach pain bloating injection site reactions (redness, pain, swelling, or irritation) breast tenderness or enlargement dizziness ovarian enlargement (abdominal or pelvic pain, tenderness, pressure, or swelling) nausea vomiting diarrhea shortness of breath pain/warmth/tenderness centralized in an arm or leg fever chills drowsiness weakness or aching of muscles or joints, or rash | Menotropins injection is used to treat infertility in women. Menotropins are a mixture of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) that are produced in the body by the pituitary gland. Menotropins injection is used in women with healthy ovaries who are enrolled in a fertility program... | Repronex is a prescription medicine used to treat the symptoms of Ovulation Induction, Assisted Reproductive Technology (ART), and Spermatogenesis. Repronex may be used alone or with other medications. | NA | FOR SUBCUTANEOUS INJECTION AND INTRAMUSCULAR INJECTION | Link | Link | NA |
| 15623 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Hormones, Hormone Substitutes, and Hormone Antagonists | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15624 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Peptide Hormones | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15625 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Peptides | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15626 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Pituitary Hormones | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15627 | Th1613 | Luteinizing hormone | >Th1613_Luteinizing_hormone APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCCVAKSYNRVTVMGGFKVENHTACHCSTCYYHKS | NA | NA | NA | NA | NA | NA | 0 | NA | NA | NA | NA | NA | NA | NA | NA | Pituitary Hormones, Anterior | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15628 | Th1614 | Mecasermin rinfabate | >Th1614_Mecasermin_rinfabate GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA | NA | NA | NA | NA | NA | Half life ranges from 10 to 16 hours with a mean of 13 hours[F4054]. Mecasermin rinfabate is said to have a longer half life than [DB01277][A176065]. | Mecasermin rinfabate is approved for severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)[A176020]. Mecasermin rinfabate is similar to [DB01277] in that both drugs contain recombinant DNA origin insulin-like growth factor 1 (IGF-1). Mecasermin rinfabate however, is already bound to recombinant DNA origin insulin-like growth factor binding protein 3 (IGFBP-3)[A12605]. The binding of IGF-1 to IGFBP-3 is said to extend the half life and reduce the clearance of IGF-1 in patients with growth hormone resistant syndromes and low levels of IGFBP-3 though this may represent <500 patients worldwide[A176065]. Mecasermin rinfabate manufactured by Insmed Incorporated under the brand name Iplex was approved by the FDA in 2005[L5722]. In 2007 Insmed withdrew their application for a marketing authorization with The European Medicines Agency[F4075]. | Mecasermin rinfabate was approved for treatment of severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)[A176020]. Severe primary IGF-1 deficiency is defined by:[FDA Label] A) height standard deviation (SD) score less than or equal to 3 SD below normal B) basal IGF-1 SD score less than or equal to 3 SD below normal C) normal or above normal levels of growth hormone In 2007, Insmed (Mecasermin rinfabate's manufacturer) made an agreement with Tercica (Mecasermin's manufacturer) that Mecasermin would no longer be available for this indication but could be developed for non short stature conditions such as severe insulin resistance, myotonic muscular dystrophy, and HIV associated adipose redistribution syndrome[A176125]. | Mecasermin rinfabate promotes vertical growth in pediatric patients in a similar fashion to [DB01277][FDA Label]. [DB01277] is a biosynthetic (recombinant DNA origin) form of human insulin-like growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth[A2324]. Growth hormones (GH) bind to growth hormone receptors (GHR) in the liver and other tissues, which stimulates the synthesis of IGF-1. In target tissues, IGF-1 activates the IGF-1 receptor, resulting in intracellular signals that stimulate growth [A2323]. Although many actions of the GH are mediated through IGF-1, the precise roles of GH and IGF-1 have not been fully elucidated. Patients with severe primary IGF-1 deficiency (Primary IGFD) fail to produce adequate levels of IGF-1, due to disruption of the GH pathway used to promote IGF-1 release (possible GH pathway disruptions include mutations in the GHR, post-GHR signaling pathway, and IGF-1 gene defects[A176065]. The structure of IGFBP-3 remains unsolved[A176309]. | Mecasermin rinfabate supplies recombinant-DNA-origin IGF-1 (rhIGF-1) bound to recombinant-DNA-origin IGFBP-3. 80% of IGF-1 is naturally bound to IGFBP-3 so the binding of rhIGF-1 to rhIGFBP-3 increases the half life of rhIGF-1 compared to [DB01277]. rhIGF-1 binds to the Type I IGF-1 receptor. This receptor exerts intra-cellular signaling activity in a number of processes involved in statural growth, including mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates, and increases in organ growth[A2324]. | Studies on carcinogenicity, genotoxicity, animal fertility, fetal development, excretion in breast milk, and use in patients over 65 years have not been performed[FDA Label]. Use in pregnant, breast feeding, or geriatric populations should be avoided as there is a lack of safety data[FDA Label]. Animal reproductive toxicity studies have shown increased incidence of abortion, post implantation loss, fewer viable fetuses, and an increase in fetal skeletal abnormalities[F4054]. Insulin-like growth factor 1 (IGF-1) without insulin-like growth factor binding protein 3 (IGFBP-3) has been shown to not be mutagenic according to the Ames test and have no affect on fertility in rats given 7 times the maximum human recommended dose based on body surface area[FDA Label]. No studies have been performed in patients with impaired renal or hepatic function however these impairments are not expected to significantly affect the pharmacokinetics of Mecasermin rinfabate[F4054]. | There is little published data on the pharmacokinetics of Mecasermin rinfabate[A12605]. Mecasermin rinfabate is expected to degrade into small peptides and amino acids[F4054]. It is suspected that IGFBP-3 in Mecasermin rinfabate is broken down by serine proteases or metalloproteases[A12605]. | There is little published data on the pharmacokinetics of Mecasermin rinfabate[A12605]. Mecasermin rinfabate is injected subcutaneously and distributes rapidly throughout the body, especially in well vascularized tissue[F4054]. | Approximately 1000mL/kg[F4054]. | Clearance ranges from 50 to 56mL/hr/kg with a mean of 53mL/hr/kg[F4054]. Mecasermin rinfabate is said to have lower clearance than [DB01277][A176065] | Anterior Pituitary Lobe Hormones and Analogues | NA | NA | NA | NA | Insulin-like growth factor 1 receptor,Insulin receptor,Cation-independent mannose-6-phosphate receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15629 | Th1614 | Mecasermin rinfabate | >Th1614_Mecasermin_rinfabate GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA | NA | NA | NA | NA | NA | Half life ranges from 10 to 16 hours with a mean of 13 hours[F4054]. Mecasermin rinfabate is said to have a longer half life than [DB01277][A176065]. | Mecasermin rinfabate is approved for severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)[A176020]. Mecasermin rinfabate is similar to [DB01277] in that both drugs contain recombinant DNA origin insulin-like growth factor 1 (IGF-1). Mecasermin rinfabate however, is already bound to recombinant DNA origin insulin-like growth factor binding protein 3 (IGFBP-3)[A12605]. The binding of IGF-1 to IGFBP-3 is said to extend the half life and reduce the clearance of IGF-1 in patients with growth hormone resistant syndromes and low levels of IGFBP-3 though this may represent <500 patients worldwide[A176065]. Mecasermin rinfabate manufactured by Insmed Incorporated under the brand name Iplex was approved by the FDA in 2005[L5722]. In 2007 Insmed withdrew their application for a marketing authorization with The European Medicines Agency[F4075]. | Mecasermin rinfabate was approved for treatment of severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)[A176020]. Severe primary IGF-1 deficiency is defined by:[FDA Label] A) height standard deviation (SD) score less than or equal to 3 SD below normal B) basal IGF-1 SD score less than or equal to 3 SD below normal C) normal or above normal levels of growth hormone In 2007, Insmed (Mecasermin rinfabate's manufacturer) made an agreement with Tercica (Mecasermin's manufacturer) that Mecasermin would no longer be available for this indication but could be developed for non short stature conditions such as severe insulin resistance, myotonic muscular dystrophy, and HIV associated adipose redistribution syndrome[A176125]. | Mecasermin rinfabate promotes vertical growth in pediatric patients in a similar fashion to [DB01277][FDA Label]. [DB01277] is a biosynthetic (recombinant DNA origin) form of human insulin-like growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth[A2324]. Growth hormones (GH) bind to growth hormone receptors (GHR) in the liver and other tissues, which stimulates the synthesis of IGF-1. In target tissues, IGF-1 activates the IGF-1 receptor, resulting in intracellular signals that stimulate growth [A2323]. Although many actions of the GH are mediated through IGF-1, the precise roles of GH and IGF-1 have not been fully elucidated. Patients with severe primary IGF-1 deficiency (Primary IGFD) fail to produce adequate levels of IGF-1, due to disruption of the GH pathway used to promote IGF-1 release (possible GH pathway disruptions include mutations in the GHR, post-GHR signaling pathway, and IGF-1 gene defects[A176065]. The structure of IGFBP-3 remains unsolved[A176309]. | Mecasermin rinfabate supplies recombinant-DNA-origin IGF-1 (rhIGF-1) bound to recombinant-DNA-origin IGFBP-3. 80% of IGF-1 is naturally bound to IGFBP-3 so the binding of rhIGF-1 to rhIGFBP-3 increases the half life of rhIGF-1 compared to [DB01277]. rhIGF-1 binds to the Type I IGF-1 receptor. This receptor exerts intra-cellular signaling activity in a number of processes involved in statural growth, including mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates, and increases in organ growth[A2324]. | Studies on carcinogenicity, genotoxicity, animal fertility, fetal development, excretion in breast milk, and use in patients over 65 years have not been performed[FDA Label]. Use in pregnant, breast feeding, or geriatric populations should be avoided as there is a lack of safety data[FDA Label]. Animal reproductive toxicity studies have shown increased incidence of abortion, post implantation loss, fewer viable fetuses, and an increase in fetal skeletal abnormalities[F4054]. Insulin-like growth factor 1 (IGF-1) without insulin-like growth factor binding protein 3 (IGFBP-3) has been shown to not be mutagenic according to the Ames test and have no affect on fertility in rats given 7 times the maximum human recommended dose based on body surface area[FDA Label]. No studies have been performed in patients with impaired renal or hepatic function however these impairments are not expected to significantly affect the pharmacokinetics of Mecasermin rinfabate[F4054]. | There is little published data on the pharmacokinetics of Mecasermin rinfabate[A12605]. Mecasermin rinfabate is expected to degrade into small peptides and amino acids[F4054]. It is suspected that IGFBP-3 in Mecasermin rinfabate is broken down by serine proteases or metalloproteases[A12605]. | There is little published data on the pharmacokinetics of Mecasermin rinfabate[A12605]. Mecasermin rinfabate is injected subcutaneously and distributes rapidly throughout the body, especially in well vascularized tissue[F4054]. | Approximately 1000mL/kg[F4054]. | Clearance ranges from 50 to 56mL/hr/kg with a mean of 53mL/hr/kg[F4054]. Mecasermin rinfabate is said to have lower clearance than [DB01277][A176065] | Pituitary and Hypothalamic Hormones and Analogues | NA | NA | NA | NA | Insulin-like growth factor 1 receptor,Insulin receptor,Cation-independent mannose-6-phosphate receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15630 | Th1614 | Mecasermin rinfabate | >Th1614_Mecasermin_rinfabate GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA | NA | NA | NA | NA | NA | Half life ranges from 10 to 16 hours with a mean of 13 hours[F4054]. Mecasermin rinfabate is said to have a longer half life than [DB01277][A176065]. | Mecasermin rinfabate is approved for severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)[A176020]. Mecasermin rinfabate is similar to [DB01277] in that both drugs contain recombinant DNA origin insulin-like growth factor 1 (IGF-1). Mecasermin rinfabate however, is already bound to recombinant DNA origin insulin-like growth factor binding protein 3 (IGFBP-3)[A12605]. The binding of IGF-1 to IGFBP-3 is said to extend the half life and reduce the clearance of IGF-1 in patients with growth hormone resistant syndromes and low levels of IGFBP-3 though this may represent <500 patients worldwide[A176065]. Mecasermin rinfabate manufactured by Insmed Incorporated under the brand name Iplex was approved by the FDA in 2005[L5722]. In 2007 Insmed withdrew their application for a marketing authorization with The European Medicines Agency[F4075]. | Mecasermin rinfabate was approved for treatment of severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)[A176020]. Severe primary IGF-1 deficiency is defined by:[FDA Label] A) height standard deviation (SD) score less than or equal to 3 SD below normal B) basal IGF-1 SD score less than or equal to 3 SD below normal C) normal or above normal levels of growth hormone In 2007, Insmed (Mecasermin rinfabate's manufacturer) made an agreement with Tercica (Mecasermin's manufacturer) that Mecasermin would no longer be available for this indication but could be developed for non short stature conditions such as severe insulin resistance, myotonic muscular dystrophy, and HIV associated adipose redistribution syndrome[A176125]. | Mecasermin rinfabate promotes vertical growth in pediatric patients in a similar fashion to [DB01277][FDA Label]. [DB01277] is a biosynthetic (recombinant DNA origin) form of human insulin-like growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth[A2324]. Growth hormones (GH) bind to growth hormone receptors (GHR) in the liver and other tissues, which stimulates the synthesis of IGF-1. In target tissues, IGF-1 activates the IGF-1 receptor, resulting in intracellular signals that stimulate growth [A2323]. Although many actions of the GH are mediated through IGF-1, the precise roles of GH and IGF-1 have not been fully elucidated. Patients with severe primary IGF-1 deficiency (Primary IGFD) fail to produce adequate levels of IGF-1, due to disruption of the GH pathway used to promote IGF-1 release (possible GH pathway disruptions include mutations in the GHR, post-GHR signaling pathway, and IGF-1 gene defects[A176065]. The structure of IGFBP-3 remains unsolved[A176309]. | Mecasermin rinfabate supplies recombinant-DNA-origin IGF-1 (rhIGF-1) bound to recombinant-DNA-origin IGFBP-3. 80% of IGF-1 is naturally bound to IGFBP-3 so the binding of rhIGF-1 to rhIGFBP-3 increases the half life of rhIGF-1 compared to [DB01277]. rhIGF-1 binds to the Type I IGF-1 receptor. This receptor exerts intra-cellular signaling activity in a number of processes involved in statural growth, including mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates, and increases in organ growth[A2324]. | Studies on carcinogenicity, genotoxicity, animal fertility, fetal development, excretion in breast milk, and use in patients over 65 years have not been performed[FDA Label]. Use in pregnant, breast feeding, or geriatric populations should be avoided as there is a lack of safety data[FDA Label]. Animal reproductive toxicity studies have shown increased incidence of abortion, post implantation loss, fewer viable fetuses, and an increase in fetal skeletal abnormalities[F4054]. Insulin-like growth factor 1 (IGF-1) without insulin-like growth factor binding protein 3 (IGFBP-3) has been shown to not be mutagenic according to the Ames test and have no affect on fertility in rats given 7 times the maximum human recommended dose based on body surface area[FDA Label]. No studies have been performed in patients with impaired renal or hepatic function however these impairments are not expected to significantly affect the pharmacokinetics of Mecasermin rinfabate[F4054]. | There is little published data on the pharmacokinetics of Mecasermin rinfabate[A12605]. Mecasermin rinfabate is expected to degrade into small peptides and amino acids[F4054]. It is suspected that IGFBP-3 in Mecasermin rinfabate is broken down by serine proteases or metalloproteases[A12605]. | There is little published data on the pharmacokinetics of Mecasermin rinfabate[A12605]. Mecasermin rinfabate is injected subcutaneously and distributes rapidly throughout the body, especially in well vascularized tissue[F4054]. | Approximately 1000mL/kg[F4054]. | Clearance ranges from 50 to 56mL/hr/kg with a mean of 53mL/hr/kg[F4054]. Mecasermin rinfabate is said to have lower clearance than [DB01277][A176065] | Somatropin and Somatropin Agonists | NA | NA | NA | NA | Insulin-like growth factor 1 receptor,Insulin receptor,Cation-independent mannose-6-phosphate receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15631 | Th1614 | Mecasermin rinfabate | >Th1614_Mecasermin_rinfabate GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA | NA | NA | NA | NA | NA | Half life ranges from 10 to 16 hours with a mean of 13 hours[F4054]. Mecasermin rinfabate is said to have a longer half life than [DB01277][A176065]. | Mecasermin rinfabate is approved for severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)[A176020]. Mecasermin rinfabate is similar to [DB01277] in that both drugs contain recombinant DNA origin insulin-like growth factor 1 (IGF-1). Mecasermin rinfabate however, is already bound to recombinant DNA origin insulin-like growth factor binding protein 3 (IGFBP-3)[A12605]. The binding of IGF-1 to IGFBP-3 is said to extend the half life and reduce the clearance of IGF-1 in patients with growth hormone resistant syndromes and low levels of IGFBP-3 though this may represent <500 patients worldwide[A176065]. Mecasermin rinfabate manufactured by Insmed Incorporated under the brand name Iplex was approved by the FDA in 2005[L5722]. In 2007 Insmed withdrew their application for a marketing authorization with The European Medicines Agency[F4075]. | Mecasermin rinfabate was approved for treatment of severe primary insulin-like growth factor (IGF) deficiency or in patients with GH gene deletion who have developed antibodies to growth hormone (GH)[A176020]. Severe primary IGF-1 deficiency is defined by:[FDA Label] A) height standard deviation (SD) score less than or equal to 3 SD below normal B) basal IGF-1 SD score less than or equal to 3 SD below normal C) normal or above normal levels of growth hormone In 2007, Insmed (Mecasermin rinfabate's manufacturer) made an agreement with Tercica (Mecasermin's manufacturer) that Mecasermin would no longer be available for this indication but could be developed for non short stature conditions such as severe insulin resistance, myotonic muscular dystrophy, and HIV associated adipose redistribution syndrome[A176125]. | Mecasermin rinfabate promotes vertical growth in pediatric patients in a similar fashion to [DB01277][FDA Label]. [DB01277] is a biosynthetic (recombinant DNA origin) form of human insulin-like growth factor 1 (IGF-1) designed to replace natural IGF-1 in pediatric patients who are deficient, promoting normalized statural growth[A2324]. Growth hormones (GH) bind to growth hormone receptors (GHR) in the liver and other tissues, which stimulates the synthesis of IGF-1. In target tissues, IGF-1 activates the IGF-1 receptor, resulting in intracellular signals that stimulate growth [A2323]. Although many actions of the GH are mediated through IGF-1, the precise roles of GH and IGF-1 have not been fully elucidated. Patients with severe primary IGF-1 deficiency (Primary IGFD) fail to produce adequate levels of IGF-1, due to disruption of the GH pathway used to promote IGF-1 release (possible GH pathway disruptions include mutations in the GHR, post-GHR signaling pathway, and IGF-1 gene defects[A176065]. The structure of IGFBP-3 remains unsolved[A176309]. | Mecasermin rinfabate supplies recombinant-DNA-origin IGF-1 (rhIGF-1) bound to recombinant-DNA-origin IGFBP-3. 80% of IGF-1 is naturally bound to IGFBP-3 so the binding of rhIGF-1 to rhIGFBP-3 increases the half life of rhIGF-1 compared to [DB01277]. rhIGF-1 binds to the Type I IGF-1 receptor. This receptor exerts intra-cellular signaling activity in a number of processes involved in statural growth, including mitogenesis in multiple tissue types, chondrocyte growth and division along cartilage growth plates, and increases in organ growth[A2324]. | Studies on carcinogenicity, genotoxicity, animal fertility, fetal development, excretion in breast milk, and use in patients over 65 years have not been performed[FDA Label]. Use in pregnant, breast feeding, or geriatric populations should be avoided as there is a lack of safety data[FDA Label]. Animal reproductive toxicity studies have shown increased incidence of abortion, post implantation loss, fewer viable fetuses, and an increase in fetal skeletal abnormalities[F4054]. Insulin-like growth factor 1 (IGF-1) without insulin-like growth factor binding protein 3 (IGFBP-3) has been shown to not be mutagenic according to the Ames test and have no affect on fertility in rats given 7 times the maximum human recommended dose based on body surface area[FDA Label]. No studies have been performed in patients with impaired renal or hepatic function however these impairments are not expected to significantly affect the pharmacokinetics of Mecasermin rinfabate[F4054]. | There is little published data on the pharmacokinetics of Mecasermin rinfabate[A12605]. Mecasermin rinfabate is expected to degrade into small peptides and amino acids[F4054]. It is suspected that IGFBP-3 in Mecasermin rinfabate is broken down by serine proteases or metalloproteases[A12605]. | There is little published data on the pharmacokinetics of Mecasermin rinfabate[A12605]. Mecasermin rinfabate is injected subcutaneously and distributes rapidly throughout the body, especially in well vascularized tissue[F4054]. | Approximately 1000mL/kg[F4054]. | Clearance ranges from 50 to 56mL/hr/kg with a mean of 53mL/hr/kg[F4054]. Mecasermin rinfabate is said to have lower clearance than [DB01277][A176065] | Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins | NA | NA | NA | NA | Insulin-like growth factor 1 receptor,Insulin receptor,Cation-independent mannose-6-phosphate receptor | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15883 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Amino Acids, Peptides, and Proteins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15884 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Anti-HIV Agents | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15885 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Anti-Infective Agents | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15886 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Anti-Retroviral Agents | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15887 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Antiviral Agents | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15888 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Biological Factors | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15889 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Chemokines, CC | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15890 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Chemotactic Factors | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15891 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Cytokines | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15892 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Inflammation Mediators | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15893 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Intercellular Signaling Peptides and Proteins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15894 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Peptides | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 15895 | Th1639 | Viral Macrophage-Inflammatory Protein | >Th1639_Viral_Macrophage-Inflammatory_Protein MDTKGILLVAVLTALLCLQSGDTLGASWHRPDKCCLGYQKRPLPQVLLSSWYPTSQLCSKPGVIFLTKRGRQVCADKSKDWVKKLMQQLPVTAR | NA | NA | NA | NA | NA | NA | Viral macrophage inflammatory protein-II (vMIP) is a highly basic protein and human chemokine analog encoded by human herpesvirus-8. The structure of vMIP consists of 71 residues and is a monomer under most conditions. It helps its virus evade the host immune system through selectively blocking and activating different receptors, preferentially inhibiting acute Th1-associated inflammation while also upregulating Th2 associated immune response. | NA | NA | This protein has the ability to bind to chemokine receptors (including both HIV coreceptors) and cell surface glycosaminoglycans. At the chemokine receptors, vMIP acts as an antagonist at CCR1, CCR2, CCR5, and CXCR4 while it is an agonist at CCR3 and CCR8. Due to its antagonistic action at CCR5 and CXCR4, vMIP is able to block HIV cell entry through these coreceptors while also inhibiting inflammation of monocytes and Th1 type T cells -- both major targets for HIV-1 and thus vMIP has potential to act as an HIV inhibitor. Glycosaminoglycans, on the other hand, are important as the binding to glycosaminoglycans may be essential for the protein to carry out its natural function in vivo. vMIP is angiogenic -- its pro-angiogenic capabilities in mature and progenitor endothelial cells gives it potential for use in organ transplantations. It is also selectively chemotactic for Th2 lymphocytes. Overall, the major role of vMIP-II is regulation of immune responses. | NA | NA | NA | NA | NA | Proteins | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 16198 | Th1711 | rhMBL | >Th1711_rhMBL MSLFPSLPLLLLSMVAASYSETVTCEDAQKTCPAVIACSSPGINGFPGKDGRDGTKGEKG | NA | NA | NA | NA | NA | NA | rhMBL is a protein therapeutic being developed by Enzon for the prevention and treatment of severe infections in individuals with low levels of Mannose-Binding Lectin (MBL). Over 10 percent of the general population is estimated to be MBL-deficient. Natural MBL is a 400-700kDa oligomer made of 3 identical 32kDa peptide chains. MBL forms different oligomers but must form at least a tetramer to be active. | Investigated for use/treatment in immunodeficiency and infectious and parasitic disease (unspecified). | NA | MBL deficiency may explain why some but not all individuals who are immunosuppressed develop infectious complications even when they receive prophylactic anti-infectious treatment. Studies have shown a correlation between low MBL levels and susceptibility to serious infections in patients immunosuppressed from chemotherapy, including patients with multiple myeloma undergoing high-dose chemotherapy and hematopoietic stem cell transplantation. rhMBL acts as natural MBL in the body, reducing susceptibility to serious infections. | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | Link | NA | NA |
| 16209 | Th1722 | ADH-1 | >Th1722_ADH-1 GLKAADNDPTAPPYDSLLVFDYEGSGSTAGSLSSLNSSSSGGDQDYDYLNDWGPRFKKLADMYGGGDD | NA | NA | NA | NA | NA | NA | Adherex's biotechnology compound, ADH-1, targets N-cadherin, a protein present on certain tumor cells and established tumor blood vessels. ADH-1 is currently in clinical development in a combination program with a range of chemotherapeutic agents to investigate the synergistic effects noted in our preclinical models. At the end of 2006, the Company also completed patient enrollment in our single-agent Phase Ib/II and Phase II trials of ADH-1. Cadherins are cell adhesion and cell signaling molecules crucial to the development of tissues, organs and organisms. Agents that target and inhibit cadherin function have the potential to attack the progression of cancer at two distinct points: * Direct targeting of cadherins expressed on cancer cells may disturb cadherin-mediated signaling, leading to apoptosis (death) of cancer cells. * Cadherin inhibitors may exploit the inherent structural weaknesses of the tumor vasculature, causing angiolysis (disruption of blood vessels) and tumor damage. As many tumors become more aggressive, invasive, and malignant, researchers have found that N-cadherin is expressed in greater amounts, making it an important target for developing anti-cancer treatments. Poorly differentiated, highly invasive carcinomas are characterized by over-expression of N-cadherin (as opposed to E-cadherin). This change in primary cadherin expression causes the epithelial cells to lose their tightly adherent, polarized and well-defined shape and become loosely adherent, flattened and migratory. Such cadherin switching promotes properties such as dedifferentiation, local invasion and metastasis, leading to poor prognosis. ADH-1 may have utility in a wide variety of cancers as N-cadherin is overexpressed in a variety of tumors. As tumors progress to become higher grade, invasive and more metastatic, the frequency of N-cadherin expression generally rises. | Investigated for use/treatment in breast cancer, cancer/tumors (unspecified), melanoma, ovarian cancer, and solid tumors. | ADH-1 is a biotech compounds that targets N-cadherin, a protein present on certain tumor cells and established tumor blood vessels. Cadherins are cell adhesion and cell signaling molecules crucial to the development of tissues, organs and organisms. Agents that target and inhibit cadherin function have the potential to attack the progression of cancer at two distinct points: * Direct targeting of cadherins expressed on cancer cells may disturb cadherin-mediated signaling, leading to apoptosis (death) of cancer cells. * Cadherin inhibitors may exploit the inherent structural weaknesses of the tumor vasculature, causing angiolysis (disruption of blood vessels) and tumor damage. The compound is indicated for treatment of a variety of invasive carcinomas and ADH-1 has been shown to be synergistic with taxane-based chemotherapy in the systemic treatment of ovarian cancer xenografts. | While ADH-1 has a single molecular target, N-cadherin, we believe its anti-cancer effect results from two distinct mechanisms of action - apoptosis and tumor vessel angiolysis. N-cadherin appears to act as a tumor cell survival factor. In cell culture studies, inhibition of N-cadherin binding between tumor cells has been shown to cause apoptosis of tumor cells, we believe as a result of disrupting the cadherin-regulated cell survival signals. ADH-1 also appears to disrupt the blood vessels needed for cancerous tumors to grow and flourish, with hemorrhaging having been noted in both our clinical and preclinical studies. We believe the mechanism for this disruption is either a competitive inhibition of the binding of cadherins between the endothelial cells of the tumor blood wall or apoptosis in tumor cells that form a part of the blood vessel wall, each leading to leakage and rupture of these vessels. The latter involves the phenomenon of tumor "mosaicism," in which tumor cells form a portion of the vascular wall (along with the endothelial cells). Induction of cell death of these tumor cells would result in tumor vascular disruption. | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | NA | (4R,7S,10S,13S,16R)-16-acetamido-13-(1H-imidazol-5-ylmethyl)-10-methyl-6,9,12,15-tetraoxo-7-propan-2-yl-1,2-dithia-5,8,11,14-tetrazacycloheptadecane-4-carboxamide | NA | Link | NA | NA |