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Identification
Name Follitropin beta
Accession Number DB00066 (BIOD00064, BIOD00099, BTD00064, BTD00099)
Type biotech
Groups approved
Description

Human follicle stimulating hormone (FSH) preparation of recombinant DNA origin, which 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.
Protein structure Db00066
Display: 3D Structure
Protein chemical formula C975H1513N267O304S26
Protein average weight 22672.9000
Sequences 
>Alpha chain
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC
VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS

>Beta chain
NSCELTNITIAIEKEECRFCISINTTWCAGYCYTRDLVYKDPARPKIQKTCTFKELVYET
VRVPGCAHHADSLYTYPVATQCHCGKCDSDSTDCTVRGLGPSYCSFGEMKE

FASTA
Synonyms
Follicle-stimulating hormone beta subunit
Follitropin alfa/beta
Follitropin beta chain precursor
FSH-B
FSH-beta
Salts Not Available
Brand names
Name Company
Follistim (Organon)
Gonal F
Gonal-F
Brand mixtures Not Available
Categories
  • Fertility Agents
CAS number 9002-68-0
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures Not Available
Pharmacology
Indication For treatment of female infertility
Pharmacodynamics Used for the treatment of female infertility, Follitropin beta or follicle stimulating hormone (FSH) stimulates ovarian follicular growth in women who do not have primary ovarian failure. FSH, the active component of Follitropin beta is the primary hormone responsible for follicular recruitment and development.
Mechanism of action Follitropin alpha is a recombinant form of endogenous follicle stimulating hormone (FSH). 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.
Absorption Not Available
Volume of distribution
  • 8 L [female subjects following intravenous administration of a 300 IU dose]
Protein binding Not Available
Metabolism Not Available
Route of elimination Not Available
Half life 2-5 hrs
Clearance
  • 0.01 1*h-1kg-1 [European women with a single intramuscular dose of 300 IU]
  • 0.01 1*h-1kg-1 [Japanese women with a single intramuscular dose of 300 IU]
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Organon usa inc
  • Emd serono inc
Packagers
Dosage forms
Form Route Strength
Injection, powder, lyophilized, for solution Intramuscular
Injection, powder, lyophilized, for solution Subcutaneous
Prices
Unit description Cost Unit
Gonal-f rff 900 unit pen 1409.62 USD ml
Follistim AQ 900unt/1.08ml Solution 1 Cartridge = 1.17ml 1366.71 USD cartridge
Follistim AQ 600unt/0.72ml Solution 0.78ml Cartridge 911.14 USD cartridge
Gonal-f 450 unit Solution Vial 733.0 USD vial
Gonal-f rff 450 unit pen 704.81 USD pen
Gonal-f rff 300 unit pen 469.87 USD pen
Follistim AQ 300unt/0.36ml Solution 0.42ml Cartridge 455.57 USD cartridge
Follistim aq 300 unit cartridge 438.05 USD cartridge
Follistim aq 150 unit vial 219.02 USD vial
Gonal-f rff 75 unit vial 117.47 USD vial
Follistim aq 75 unit vial 109.51 USD vial
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Patents
Country Patent Number Approved Expires (estimated)
United States 7741268 2004-04-02 2024-04-02
United States 5270057 1994-03-20 2011-03-20
Canada 2037884 2003-10-21 2011-03-08
Properties
State liquid
Experimental Properties
Property Value Source
melting point 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
References
Synthesis Reference Not Available
General Reference
  1. Goa KL, Wagstaff AJ: Follitropin alpha in infertility: a review. BioDrugs. 1998 Mar;9(3):235-60. Pubmed
External Links
Resource Link
UniProt P01225 Link_out
Genbank M16647 Link_out
PharmGKB PA449693 Link_out
Drug Product Database 2243949 Link_out
RxList http://www.rxlist.com/cgi/generic3/follitrop.htm Link_out
Drugs.com http://www.drugs.com/cdi/follitropin-alfa-powder.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Follicle-stimulating_hormone Link_out
ATC Codes
  • G03GA06
AHFS Codes Not Available
PDB Entries
FDA label show (468 KB)
MSDS Not Available
Interactions
Drug Interactions Searched, but no interactions found.
Food Interactions Not Available
Targets

1. Follicle-stimulating hormone receptor

Pharmacological action: yes
Actions: agonist

Receptor for follicle-stimulating hormone. The activity of this receptor is mediated by G proteins which activate adenylate cyclase

Organism class: human
UniProt ID: P23945 Link_out
Gene: FSHR Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

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
  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
  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
  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
  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
  6. Goa KL, Wagstaff AJ: Follitropin alpha in infertility: a review. BioDrugs. 1998 Mar;9(3):235-60. Pubmed
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on September 03, 2011 16:42