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Accession NumberDB00106  (BIOD00051, BTD00051)
GroupsApproved, Investigational, Withdrawn

Synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It is marketed by Praecis Pharmaceuticals as Plenaxis. Praecis announced in June 2006 that it was voluntarily withdrawing the drug from the market.

Protein structureDb00106
Protein chemical formulaC72H95ClN14O14
Protein average weight1416.0630
SynonymsNot Available
External Identifiers Not Available
Prescription ProductsNot Available
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
PlenaxisPraecis Pharmaceuticals
Brand mixturesNot Available
SaltsNot Available
CAS number183552-38-7
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
IndicationFor palliative treatment of advanced prostate cancer.
PharmacodynamicsUsed in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis.
Mechanism of actionAbarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.
AbsorptionFollowing IM administration of 100 mg, abarelix is absorbed slowly with a mean peak concentration of 43.4 ng/mL observed approximately 3 days after the injection.
Volume of distributionNot Available
Protein binding96-99%

In vitro hepatocyte (rat, monkey, human) studies and in vivo studies in rats and monkeys showed that the major metabolites of abarelix were formed via hydrolysis of peptide bonds. No significant oxidative or conjugated metabolites of abarelix were found either in vitro or in vivo. There is no evidence of cytochrome P-450 involvement in the metabolism of abarelix.

Route of eliminationNot Available
Half life13.2 ± 3.2 days
ClearanceNot Available
ToxicityThe maximum tolerated dose of abarelix has not been determined. The maximum dose used in clinical studies was 150 mg. There have been no reports of accidental overdose with abarelix.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
  • Speciality european pharma ltd
Dosage formsNot Available
PricesNot Available
CountryPatent NumberApprovedExpires (estimated)
United States59688951996-12-112016-12-11
United States64236861995-06-072015-06-07
Experimental PropertiesNot Available
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesL02BX01
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (121 KB)
MSDSNot Available
Drug InteractionsNot Available
Food InteractionsNot Available


1. Gonadotropin-releasing hormone receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist


Name UniProt ID Details
Gonadotropin-releasing hormone receptor P30968 Details


  1. Debruyne FM: Gonadotropin-releasing hormone antagonist in the management of prostate cancer. Rev Urol. 2004;6 Suppl 7:S25-32. Pubmed

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Drug created on June 13, 2005 07:24 /Updated on August 07, 2014 11:05