Urofollitropin
Identification
- Summary
Urofollitropin is a form of purified human follicle stimulating hormone used to treat infertility in females by inducing follicle development in women without primary ovarian failure.
- Generic Name
- Urofollitropin
- DrugBank Accession Number
- DB00094
- Background
Urofollitropin is a urinary-derived follicle-stimulating hormone (FSH) that is extracted and purified from human urine samples. 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 typically used injected subcutaneously in combination with human chorionic gonadotropin (hCG) to induce ovulation. 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).
- Type
- Biotech
- Groups
- Approved, Vet approved
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Structure
- Protein Chemical Formula
- C42H65N11O12S2
- Protein Average Weight
- 980.162 Da
- Sequences
>Alpha chain APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS
>Beta chain NSCELTNITIAIEKEECRFCISINTTWCAGYCYTRDLVYKDPARPKIQKTCTFKELVYET VRVPGCAHHADSLYTYPVATQCHCGKCDSDSTDCTVRGLGPSYCSFGEMKE
Download FASTA Format- Synonyms
- Follitropin human
- Urofollitrophin
- Urofollitropin
Pharmacology
- Indication
For treatment of female infertility
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- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Used for the 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.
- 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.
Target Actions Organism AFollicle-stimulating hormone receptor agonistHumans - Absorption
74%
- Volume of distribution
Time to peak in plasma: IM: 17 hours (single dose), 11 hours (multiple doses) SubQ: 21 hours (single dose), 10 hours (multiple doses)
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Via liver and kidneys
- Half-life
Circulation half life of 3-4 hours, elimination half life of 35-40 hours
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.No interactions found.
- Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- International/Other Brands
- Fertinex (Serono S.A.) / Metrodin (Serum Inst.)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Bravelle Powder, for solution 75 unit / vial Intramuscular; Subcutaneous Ferring Pharmaceuticals 2005-06-15 2019-07-18 Canada Metrodin 75 I.U. Powder, for solution 75 unit / amp Intramuscular Industria Farmaceutica Serono Spa 1988-12-31 1999-08-11 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Fertinorm Hp 150 - Pws Diluent Im Sc Urofollitropin (150 unit / vial) + Sodium chloride (2 mL / vial) Kit; Liquid; Powder, for solution Intramuscular; Subcutaneous Emd Serono, A Division Of Emd Inc., Canada 1994-12-31 2007-05-07 Canada Fertinorm Hp 75 - Pws Diluent Im Sc Urofollitropin (75 unit / kit) + Sodium chloride (2 mL / kit) Liquid; Powder, for solution Intramuscular; Subcutaneous Emd Serono, A Division Of Emd Inc., Canada 1994-12-31 2007-05-07 Canada
Categories
- ATC Codes
- G03GA04 — Urofollitropin
- Drug Categories
- Amino Acids, Peptides, and Proteins
- 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
- Sex Hormones and Modulators of the Genital System
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- W9BB98U6HP
- CAS number
- 97048-13-0
References
- General References
- Goa KL, Wagstaff AJ: Follitropin alpha in infertility: a review. BioDrugs. 1998 Mar;9(3):235-60. [Article]
- External Links
- UniProt
- P01225
- Genbank
- M16647
- PubChem Substance
- 46507385
- 134404
- ChEMBL
- CHEMBL1201520
- Therapeutic Targets Database
- DAP001029
- PharmGKB
- PA451835
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Urofollitropin
- FDA label
- Download (174 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Health Services Research Female Infertility 1 4 Completed Treatment Infertility 4 4 Not Yet Recruiting Treatment Female Infertility 1 4 Recruiting Treatment Infertility 1 4 Unknown Status Treatment IVF 1
Pharmacoeconomics
- Manufacturers
- Serono laboratories inc
- Ferring pharmaceuticals inc
- Packagers
- Cardinal Health
- Draxis Specialty Pharmaceuticals Inc.
- Ferring Pharmaceuticals Inc.
- Instituto Massone SA
- Merck Serono SPA
- North America Genescience LLC
- Organon Pharmaceuticals
- Serono SA
- Vetter Pharma Fertigung GmbH and Co. KG
- Dosage Forms
Form Route Strength Powder, for solution Powder, for solution Intramuscular; Subcutaneous 75 unit / vial Solution Parenteral 75 UI Injection, powder, for solution Subcutaneous Injection, powder, for solution Subcutaneous 75 IU Kit; liquid; powder, for solution Intramuscular; Subcutaneous Liquid; powder, for solution Intramuscular; Subcutaneous Injection, powder, lyophilized, for solution Intramuscular; Subcutaneous Injection, powder, for solution Parenteral 150 UI/ML Injection, powder, for solution Parenteral 75 UI/ML Injection, powder, for solution Parenteral; Subcutaneous 225 UI/1ML Injection, powder, for solution Parenteral; Subcutaneous 300 UI/1ML Powder, for solution 150 UI/ML Injection, powder, for solution Parenteral Injection 150 iu Injection, powder, lyophilized, for solution Intramuscular; Subcutaneous 150 IU Injection 75 iu Injection, powder, lyophilized, for solution Intramuscular; Subcutaneous 75 IU Injection, powder, for solution Parenteral 150 I.E. Injection, powder, for solution Parenteral 75 I.E. Powder, for solution Intramuscular 75 unit / amp - Prices
Unit description Cost Unit Fertinex 75 unit Solution 103.85USD vial Bravelle 75 unit vial 93.85USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5767067 No 1998-06-16 2015-06-16 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 55 °C Forastieri, H., Ingham, K.C. J. Biol. Chem. 257:7976-7981 (1982) hydrophobicity -0.330 Not Available isoelectric point 7.50 Not Available
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- G-protein coupled peptide receptor activity
- Specific Function
- Receptor for follicle-stimulating hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Induces cAMP production through the activation of PI3K-AKT and S...
- Gene Name
- FSHR
- Uniprot ID
- P23945
- Uniprot Name
- Follicle-stimulating hormone receptor
- Molecular Weight
- 78264.07 Da
References
- Layman LC: Mutations in the follicle-stimulating hormone-beta (FSH beta) and FSH receptor genes in mice and humans. Semin Reprod Med. 2000;18(1):5-10. [Article]
- Leng N, Dattatreyamurty B, Reichert LE Jr: Identification of amino acid residues 300-315 of the rat FSH receptor as a hormone binding domain: evidence for its interaction with specific regions of FSH beta-subunit. Biochem Biophys Res Commun. 1995 May 16;210(2):392-9. [Article]
- Santa Coloma TA, Dattatreyamurty B, Reichert LE Jr: A synthetic peptide corresponding to human FSH beta-subunit 33-53 binds to FSH receptor, stimulates basal estradiol biosynthesis, and is a partial antagonist of FSH. Biochemistry. 1990 Feb 6;29(5):1194-200. [Article]
- Dattatreyamurty B, Reichert LE Jr: Identification of regions of the follitropin (FSH) beta-subunit that interact with the N-terminus region (residues 9-30) of the FSH receptor. Mol Cell Endocrinol. 1993 May;93(1):39-46. [Article]
- Lindau-Shepard B, Roth KE, Dias JA: Identification of amino acids in the C-terminal region of human follicle-stimulating hormone (FSH) beta-subunit involved in binding to human FSH receptor. Endocrinology. 1994 Sep;135(3):1235-40. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55