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Identification
NameFollitropin beta
Accession NumberDB00066  (BTD00099, BTD00064, BIOD00099, BIOD00064)
TypeBiotech
GroupsApproved
DescriptionFollitropin beta is a 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. The alpha subunit is glycosylated at Asn 51 and Asn 78 while the beta subunit is glycosylated at Asn 7 and Asn 24. Follitropin beta is produced in genetically engineered Chinese hamster cell lines (CHO). The nomenclature “beta” differentiates it from another recombinant human FSH product that was marketed earlier as follitropin alpha. Follitropin 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. Follitropin 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). Numerous physio-chemical tests and bioassays indicate that follitropin beta and follitropin alpha are indistinguishable. However, a more recent study showed there is may be a slight clinical difference, with the alpha form tending towards a higher pregnancy rate and the beta form tending towards a lower pregnancy rate, but with significantly higher estradiol (E2) levels. Structural analysis shows that the amino acid sequence of follitropin beta is identical to that of natural human follicle stimulating hormone (FSH). Further, the ogliosaccharide side chains are very similar, but not completely identical to that of natural FSH. However, these small differences do not affect the bioactivity compared to natural FSH.
Protein structureDb00066
Related Articles
Protein chemical formulaC975H1513N267O304S26
Protein average weight22672.9 Da
Sequences
>Alpha chain
APDVQDCPECTLQENPFFSQPGAPILQCMGCCFSRAYPTPLRSKKTMLVQKNVTSESTCC
VAKSYNRVTVMGGFKVENHTACHCSTCYYHKS
>Beta chain
NSCELTNITIAIEKEECRFCISINTTWCAGYCYTRDLVYKDPARPKIQKTCTFKELVYET
VRVPGCAHHADSLYTYPVATQCHCGKCDSDSTDCTVRGLGPSYCSFGEMKE
Download FASTA Format
Synonyms
Follicle stimulating hormone beta
Follicle-stimulating hormone beta subunit
Follitrophin beta
Follitropin beta
Follitropin beta chain precursor
FSH-b
FSH-B
FSH-beta
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
FertavidInjection, solution100 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution200 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution150 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution75 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution900 IU/1.08mLSubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution100 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution50 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution150 IU/0.18mLSubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution150 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution75 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution100 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution50 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution300 IU/0.36mLSubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution200 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution75 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution150 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution50 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution600 IU/0.72mLSubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
FertavidInjection, solution200 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Ltd  2009-03-19Not applicableEu
Follistim AQInjection, solution650 [iU]/.78mLSubcutaneousOrganon USA Inc.2004-03-24Not applicableUs
Follistim AQInjection, solution75 [iU]/.5mLIntramuscular; SubcutaneousOrganon USA Inc.2010-06-28Not applicableUs
Follistim AQInjection, solution975 [iU]/1.17mLSubcutaneousOrganon USA Inc.2004-03-24Not applicableUs
Follistim AQInjection, solution150 [iU]/.5mLIntramuscular; SubcutaneousOrganon USA Inc.2010-06-28Not applicableUs
Follistim AQInjection, solution350 [iU]/.42mLSubcutaneousOrganon USA Inc.2004-03-24Not applicableUs
PuregonInjection, solution200 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution100 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonSolution50 unitIntramuscular; SubcutaneousMerck Canada Inc2001-10-24Not applicableCanada
PuregonInjection, solution900 IU/1.08mLSubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution225 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution50 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution150 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution200 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution100 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonSolution100 unitIntramuscular; SubcutaneousMerck Canada Inc2001-10-24Not applicableCanada
PuregonInjection, solution75 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution300 IU/0.36mLSubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution150 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution225 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution50 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution100 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonSolution833 unitSubcutaneousMerck Canada Inc2001-10-18Not applicableCanada
PuregonInjection, solution75 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution600 IU/0.72mLSubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution200 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution225 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution50 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution150 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution75 IU/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
PuregonInjection, solution150 IU/0.18mLSubcutaneousMerck Sharp & Dohme Limited1996-05-03Not applicableEu
Puregon (600 Iu)Solution737 unitSubcutaneousOrganon Canada Ltd Ltee2001-10-182005-07-07Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
FollistimOrganon
Brand mixtures
NameLabellerIngredients
Puregon 100 I.U.Organon Canada Ltd Ltee
Puregon 50 I.U.Organon Canada Ltd Ltee
SaltsNot Available
Categories
UNII8FYM5179QJ
CAS number9002-68-0
Pharmacology
IndicationFor treatment of female infertility
Structured Indications Not Available
PharmacodynamicsUsed 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 actionFollitropin 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Follicle-stimulating hormone receptorProteinyes
agonist
HumanP23945 details
Related Articles
Absorption74%
Volume of distribution
  • 8 L [female subjects following intravenous administration of a 300 IU dose]
Protein bindingNot Available
MetabolismNot Available
Route of eliminationVia liver and kidneys
Half lifeCirculation half life of 3-4 hours, elimination half life of 35-40 hours
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]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug InteractionsNo interactions found.
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Goa KL, Wagstaff AJ: Follitropin alpha in infertility: a review. BioDrugs. 1998 Mar;9(3):235-60. [PubMed:18020563 ]
External Links
ATC CodesG03GA06
AHFS CodesNot Available
PDB Entries
FDA labelDownload (468 KB)
MSDSNot Available
Pharmacoeconomics
Manufacturers
  • Organon usa inc
  • Emd serono inc
Packagers
Dosage forms
FormRouteStrength
Injection, solutionIntramuscular; Subcutaneous150 [iU]/.5mL
Injection, solutionIntramuscular; Subcutaneous75 [iU]/.5mL
Injection, solutionSubcutaneous350 [iU]/.42mL
Injection, solutionSubcutaneous650 [iU]/.78mL
Injection, solutionSubcutaneous975 [iU]/1.17mL
Injection, solutionIntramuscular; Subcutaneous100 IU/0.5mL
Injection, solutionIntramuscular; Subcutaneous150 IU/0.5mL
Injection, solutionIntramuscular; Subcutaneous200 IU/0.5mL
Injection, solutionIntramuscular; Subcutaneous225 IU/0.5mL
Injection, solutionIntramuscular; Subcutaneous50 IU/0.5mL
Injection, solutionIntramuscular; Subcutaneous75 IU/0.5mL
Injection, solutionSubcutaneous150 IU/0.18mL
Injection, solutionSubcutaneous300 IU/0.36mL
Injection, solutionSubcutaneous600 IU/0.72mL
Injection, solutionSubcutaneous900 IU/1.08mL
SolutionIntramuscular; Subcutaneous100 unit
SolutionIntramuscular; Subcutaneous50 unit
SolutionSubcutaneous833 unit
SolutionSubcutaneous737 unit
Liquid; powder, for solutionIntramuscular; Subcutaneous
Prices
Unit descriptionCostUnit
Gonal-f rff 900 unit pen1409.62USD ml
Follistim AQ 900unt/1.08ml Solution 1 Cartridge = 1.17ml1366.71USD cartridge
Follistim AQ 600unt/0.72ml Solution 0.78ml Cartridge911.14USD cartridge
Gonal-f 450 unit Solution Vial733.0USD vial
Gonal-f rff 450 unit pen704.81USD pen
Gonal-f rff 300 unit pen469.87USD pen
Follistim AQ 300unt/0.36ml Solution 0.42ml Cartridge455.57USD cartridge
Follistim aq 300 unit cartridge438.05USD cartridge
Follistim aq 150 unit vial219.02USD vial
Gonal-f rff 75 unit vial117.47USD vial
Follistim aq 75 unit vial109.51USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2037884 No2003-10-212011-03-08Canada
US5270057 No1994-03-202011-03-20Us
US5929028 No1998-01-142018-01-14Us
US7446090 No1999-08-232019-08-23Us
US7563763 No1999-08-232019-08-23Us
US7741268 No2004-04-022024-04-02Us
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point55 °CForastieri, H., Ingham, K.C. J. Biol. Chem. 257:7976-7981 (1982)
hydrophobicity-0.330Not Available
isoelectric point7.50Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot 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 SRC-ERK1/2 signaling pathways.
Gene Name:
FSHR
Uniprot ID:
P23945
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. Goa KL, Wagstaff AJ: Follitropin alpha in infertility: a review. BioDrugs. 1998 Mar;9(3):235-60. [PubMed:18020563 ]
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on December 03, 2016 02:44