Identification

Name
Urofollitropin
Accession Number
DB00094  (BTD00104, BIOD00104)
Type
Biotech
Groups
Approved, Vet Approved
Biologic Classification
Protein Based Therapies
Hormones
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).

Protein structure
Db00094
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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BravelleKitSubcutaneousFerring Pharmaceuticals2002-05-06Not applicableUs
BravellePowder, for solution75 unitIntramuscular; SubcutaneousFerring Pharmaceuticals2005-06-15Not applicableCanada
Metrodin 75 I.U.Powder, for solution75 unitIntramuscularIndustria Farmaceutica Serono Spa1988-12-311999-08-11Canada
International/Other Brands
Fertinex (Serono S.A.) / Metrodin (Serum Inst.)
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Fertinorm Hp 150 - Pws Diluent Im ScUrofollitropin (150 unit) + Sodium Chloride (2 ml)Kit; Liquid; Powder, for solutionIntramuscular; SubcutaneousEmd Serono, A Division Of Emd Inc., Canada1994-12-312007-05-07Canada
Fertinorm Hp 75 - Pws Diluent Im ScUrofollitropin (75 unit) + Sodium Chloride (2 ml)Liquid; Powder, for solutionIntramuscular; SubcutaneousEmd Serono, A Division Of Emd Inc., Canada1994-12-312007-05-07Canada
Humegon Inj 75 I.U.Urofollitropin (75 unit) + Lutropin alfa (75 unit) + Sodium Chloride (.9 %)Liquid; Powder, for solutionIntramuscularOrganon Canada Ltd Ltee1993-12-312006-08-17Canada
Pergonal 75 I.U.Urofollitropin (75 unit) + Lutropin alfa (75 unit)Powder, for solutionIntramuscularEmd Serono, A Division Of Emd Inc., Canada1979-12-312007-05-07Canada
Categories
UNII
W9BB98U6HP
CAS number
97048-13-0

Pharmacology

Indication

For treatment of female infertility

Structured Indications
Not Available
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
Human
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
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
No interactions found.
Food Interactions
Not Available

References

Synthesis Reference
Not Available
General References
  1. Goa KL, Wagstaff AJ: Follitropin alpha in infertility: a review. BioDrugs. 1998 Mar;9(3):235-60. [PubMed:18020563]
  2. Link [Link]
External Links
UniProt
P01225
Genbank
M16647
ChEMBL
CHEMBL1201520
Therapeutic Targets Database
DAP001029
PharmGKB
PA451835
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Urofollitropin
ATC Codes
G03GA04 — Urofollitropin
AHFS Codes
  • 68:18.00
PDB Entries
FDA label
Download (174 KB)
MSDS
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Not Yet RecruitingTreatmentSub-fertility1
1, 2Enrolling by InvitationTreatmentFemale Infertility Due to Diminished Ovarian Reserve1
1, 2RecruitingTreatmentInfertilities1
2CompletedTreatmentInfertilities1
2TerminatedTreatmentHypogonadism / Olfacto genital dysplasia1
2TerminatedTreatmentOvulation induction therapy1
3CompletedTreatmentAnovulatory cycle1
3CompletedTreatmentAssisted Reproductive Technology therapy1
3CompletedTreatmentEmbryo Transfer / Luteal Hormone Supplementation in In-vitro Fertilization1
3CompletedTreatmentInfertilities4
3CompletedTreatmentInfertilities / Ovulation induction therapy1
3CompletedTreatmentInfertility; Oocytes Donation; Immunogenicity / Oocyte Donation1
3CompletedTreatmentPregnancy / Unexplained Infertility1
3CompletedTreatmentSubfertility1
3RecruitingTreatmentInfertilities1
3RecruitingTreatmentMale Infertility1
3SuspendedTreatmentInfertilities1
3Unknown StatusTreatmentAzoospermia1
4Active Not RecruitingTreatmentInfertilities1
4CompletedTreatmentIdiopathic Hypogonadotropic Hypogonadism / Olfacto genital dysplasia1
4CompletedTreatmentInfertilities3
Not AvailableCompletedNot AvailableInfertilities1
Not AvailableCompletedNot AvailableNeonates / Pregnancy1
Not AvailableCompletedDiagnosticHealthy Volunteers / Premature Ovarian Failure (POF)1
Not AvailableCompletedScreeningOther Diseases or Conditions1
Not AvailableCompletedTreatmentFertility1
Not AvailableCompletedTreatmentInfertilities2
Not AvailableRecruitingTreatmentInfertilities / Reproductive Techniques, Assisted1
Not AvailableUnknown StatusNot AvailableSubfertility1

Pharmacoeconomics

Manufacturers
  • Serono laboratories inc
  • Ferring pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
KitSubcutaneous
Powder, for solutionIntramuscular; Subcutaneous75 unit
Kit; liquid; powder, for solutionIntramuscular; Subcutaneous
Liquid; powder, for solutionIntramuscular; Subcutaneous
Liquid; powder, for solutionIntramuscular
Powder, for solutionIntramuscular75 unit
Powder, for solutionIntramuscular
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)
US5767067No1995-06-162015-06-16Us

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

Taxonomy

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

Targets

Kind
Protein
Organism
Human
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. [PubMed:11299519]
  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. [PubMed:7755615]
  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. [PubMed:2108722]
  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. [PubMed:8319832]
  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. [PubMed:8070368]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Drug created on June 13, 2005 07:24 / Updated on June 21, 2017 16:43