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Th1077 details
Primary information
ID1439
ThPP IDTh1077
Therapeutic Peptide/Protein NameUrofollitropin
SequenceAlpha chain:APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYP view full sequnce in fasta
Functional ClassificationIb
Molecular Weight980.162
Chemical FormulaC42H65N11O12S2
Isoelectric Point7.5
Hydrophobicity-0.33
Melting Point (℃)55
Half LifeCirculation half life of 3-4 hours, elimination half life of 35-40 hours
DescriptionUrofollitropin 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).
Indication/DiseaseFor treatment of female infertility
PharmacodynamicsUrofollitropin 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.
Mechanism of ActionFSH 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.
ToxicityN.A.
MetabolismN.A.
Absorption74%
Volume of DistributionN.A.
ClearanceN.A.
CategoriesFertility Agents
Patents NumberUS5767067
Date of Issue17/06/99
Date of Expiry17/06/19
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameBRAVELLE
CompanyFerring Pharmaceuticals Inc.
Brand DiscriptionBRAVELLE is a product containing a highly purified preparation of human follicle stimulating hormone (hFSH) extracted from the urine ofpostmenopausal 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 ofcarbohydrates. The β subunit has 111 amino acids of which two are modified by attachment of carbohydrates.
Prescribed forBRAVELLE (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
Chemical NameN.A.
FormulationEach 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.
Physcial AppearanceBRAVELLE is a sterile, lyophilized powder used after reconstitution with Sterile 0.9% Sodium Chloride Injection, USP
Route of AdministrationIntramuSubcutaneousular and Subcutaneous administr
Recommended DosageInitial 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.
ContraindicationRAVELLE 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.
Side EffectsThe 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.
Useful Linkhttp://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9bb87daf-d156-504e-adaf-4c21383f8d16 http://www.rxlist.com/bravelle-drug.htm
PubMed ID18020563
3-D StructureTh1077 (View) or (Download)
Primary information
ID1440
ThPP IDTh1077
Therapeutic Peptide/Protein NameUrofollitropin
SequenceAlpha chain:APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYP view full sequnce in fasta
Functional ClassificationIb
Molecular Weight980.162
Chemical FormulaC42H65N11O12S2
Isoelectric Point7.5
Hydrophobicity-0.33
Melting Point (℃)55
Half LifeCirculation half life of 3-4 hours, elimination half life of 35-40 hours
DescriptionUrofollitropin 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).
Indication/DiseaseFor treatment of female infertility
PharmacodynamicsUrofollitropin 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.
Mechanism of ActionFSH 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.
ToxicityN.A.
MetabolismN.A.
Absorption174%
Volume of DistributionN.A.
ClearanceN.A.
CategoriesFertility Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetGlutamate carboxypeptidase 2
Information of corresponding available drug in the market
Brand NameMetrodin
CompanyN.A.
Brand DiscriptionMetrodin (urofollitropin for injection) is a preparation of gonadotropin extracted from the urine of postmenopausal women
Prescribed forMetrodin (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.
Chemical NameN.A.
FormulationEach 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 
Physcial AppearanceMetrodin (urofollitropin for injection) is a sterile, lypholized powder form contains an acidic, water soluble glycoprotein biologically standardized for FSH gonadotropin activity
Route of AdministrationIntramuSubcutaneousular Injection.
Recommended DosageInitial starting 75 International Units per day for 5 days administered intramuscularly in polycystic ovary syndrome. In ART the dose is 150 IU per day.
Contraindicationcontraindicated 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.
Side EffectsPulmonary 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.
Useful Linkhttp://www.rxlist.com/metrodin-drug.htm
PubMed ID18020563
3-D StructureTh1077 (View) or (Download)
Primary information
ID1441
ThPP IDTh1077
Therapeutic Peptide/Protein NameUrofollitropin
SequenceAlpha chain:APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYP view full sequnce in fasta
Functional ClassificationIb
Molecular Weight980.162
Chemical FormulaC42H65N11O12S2
Isoelectric Point7.5
Hydrophobicity-0.33
Melting Point (℃)55
Half LifeCirculation half life of 3-4 hours, elimination half life of 35-40 hours
DescriptionUrofollitropin 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).
Indication/DiseaseFor treatment of female infertility
PharmacodynamicsUrofollitropin 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.
Mechanism of ActionFSH 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.
ToxicityN.A.
MetabolismN.A.
Absorption274%
Volume of DistributionN.A.
ClearanceN.A.
CategoriesFertility Agents
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameFertinex
CompanyN.A.
Brand DiscriptionFertinex (urofollitropin for injection, purified) is a preparation of highly purified Follicle Stimulating Hormone (FSH) extracted from the urine of post-menopausal women. Purification is by immunoaffinity chromatography using murine monoclonal antibody to human FSH. The purification process results in a consistent FSH isoform profile, significantly enhanced specific activity (8,500-13, 500 IU FSH/mg protein), and ≥95% purity
Prescribed forFertinexTM (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.
Chemical NameN.A.
FormulationEach 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. 
Physcial AppearanceFertinex (urofollitropin) in asterile, lyophilized powder form contains an acidic, water soluble glycoprotein biologically standardized for FSH gonadotropin activity
Route of AdministrationSubcutaneous Injection.
Recommended DosageInitial starting 75 International Units per day for 5 days administered intramuscularly in polycystic ovary syndrome. In ART the dose is 150 IU per day.
Contraindicationcontraindicated 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.
Side EffectsPulmonary 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.
Useful Linkhttp://www.rxlist.com/fertinex-drug.htm
PubMed ID18020563
3-D StructureTh1077 (View) or (Download)