| Primary information |
|---|
| ThPP ID | Th1077 |
| Therapeutic Peptide/Protein Name | Urofollitropin |
| Sequence | Alpha chain:APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYP view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 980.162 |
| Chemical Formula | C42H65N11O12S2 |
| Isoelectric Point | 7.5 |
| Hydrophobicity | -0.33 |
| Melting Point (℃) | 55 |
| Half Life | Circulation half life of 3-4 hours, elimination half life of 35-40 hours |
| Description | 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). |
| Indication/Disease | For treatment of female infertility |
| Pharmacodynamics | 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. |
| Mechanism of Action | 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. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | 74% |
| Volume of Distribution | N.A. |
| Clearance | N.A. |
| Categories | Fertility Agents |
| Patents Number | US5767067 |
| Date of Issue | 17/06/99 |
| Date of Expiry | 17/06/19 |
| Drug Interaction | N.A. |
| Target | N.A. |
| Information of corresponding available drug in the market |
|---|
| Brand Name | BRAVELLE |
| Company | Ferring Pharmaceuticals Inc. |
| Brand Discription | BRAVELLE 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 for | 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 |
| Chemical Name | N.A. |
| Formulation | 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. |
| Physcial Appearnce | BRAVELLE is a sterile, lyophilized powder used after reconstitution with Sterile 0.9% Sodium Chloride Injection, USP |
| Route of Administration | IntramuSubcutaneousular and Subcutaneous administr |
| Recommended Dosage | 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. |
| Contraindication | RAVELLEÂ 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 Effects | 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. |
| Useful Link | http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9bb87daf-d156-504e-adaf-4c21383f8d16 http://www.rxlist.com/bravelle-drug.htm |
| PubMed ID | 18020563 |
| 3-D Structure | Th1077 (View) or (Download) |