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

Reduce drug development failure rates
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Associated Therapies
Contraindications & Blackbox Warnings
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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.

TargetActionsOrganism
AFollicle-stimulating hormone receptor
agonist
Humans
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
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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

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International/Other Brands
Fertinex (Serono S.A.) / Metrodin (Serum Inst.)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BravellePowder, for solution75 unit / vialIntramuscular; SubcutaneousFerring Pharmaceuticals2005-06-152019-07-18Canada flag
Metrodin 75 I.U.Powder, for solution75 unit / ampIntramuscularIndustria Farmaceutica Serono Spa1988-12-311999-08-11Canada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Fertinorm Hp 150 - Pws Diluent Im ScUrofollitropin (150 unit / vial) + Sodium chloride (2 mL / vial)Kit; Liquid; Powder, for solutionIntramuscular; SubcutaneousEmd Serono, A Division Of Emd Inc., Canada1994-12-312007-05-07Canada flag
Fertinorm Hp 75 - Pws Diluent Im ScUrofollitropin (75 unit / kit) + Sodium chloride (2 mL / kit)Liquid; Powder, for solutionIntramuscular; SubcutaneousEmd Serono, A Division Of Emd Inc., Canada1994-12-312007-05-07Canada flag

Categories

ATC Codes
G03GA04 — Urofollitropin
Drug Categories
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
  1. Goa KL, Wagstaff AJ: Follitropin alpha in infertility: a review. BioDrugs. 1998 Mar;9(3):235-60. [Article]
UniProt
P01225
Genbank
M16647
PubChem Substance
46507385
RxNav
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
PhaseStatusPurposeConditionsCount
4CompletedHealth Services ResearchFemale Infertility1
4CompletedTreatmentInfertility4
4Not Yet RecruitingTreatmentFemale Infertility1
4RecruitingTreatmentInfertility1
4RecruitingTreatmentIVF1
3CompletedTreatmentAnovulatory cycle1
3CompletedTreatmentFemale Infertility1
3CompletedTreatmentInfertility2
3CompletedTreatmentInfertility / Ovulation induction therapy1
3CompletedTreatmentSubfertility1

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
FormRouteStrength
Powder, for solution
Powder, for solutionIntramuscular; Subcutaneous75 unit / vial
Injection, powder, for solutionSubcutaneous
Injection, powder, for solutionSubcutaneous75 IU
Kit; liquid; powder, for solutionIntramuscular; Subcutaneous
Liquid; powder, for solutionIntramuscular; Subcutaneous
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous
Injection, powder, lyophilized, for solutionIntramuscular; Subcutaneous75 IU
Injection, powder, for solutionParenteral150 UI/ML
Injection, powder, for solutionParenteral75 UI/ML
Injection, powder, for solutionParenteral; Subcutaneous225 UI/1ML
Injection, powder, for solutionParenteral; Subcutaneous300 UI/1ML
Powder, for solution150 UI/ML
Injection, powder, for solutionParenteral
Injection
Injection, powder, for solutionParenteral150 I.E.
Injection, powder, for solutionParenteral75 I.E.
Powder, for solutionIntramuscular75 unit / amp
Prices
Unit descriptionCostUnit
Fertinex 75 unit Solution103.85USD vial
Bravelle 75 unit vial93.85USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5767067No1998-06-162015-06-16US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)55 °CForastieri, H., Ingham, K.C. J. Biol. Chem. 257:7976-7981 (1982)
hydrophobicity-0.330Not Available
isoelectric point7.50Not Available

Targets

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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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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 June 26, 2022 10:21