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Identification
NameAbarelix
Accession NumberDB00106  (BTD00051, BIOD00051)
TypeBiotech
GroupsApproved, Investigational, Withdrawn
DescriptionSynthetic 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
Related Articles
Protein chemical formulaC72H95ClN14O14
Protein average weight1416.063 Da
SequencesNot Available
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PlenaxisPraecis Pharmaceuticals
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIW486SJ5824
CAS number183552-38-7
Pharmacology
IndicationFor palliative treatment of advanced prostate cancer.
Structured Indications Not Available
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Gonadotropin-releasing hormone receptorProteinyes
antagonist
HumanP30968 details
Related Articles
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%
Metabolism

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
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesL02BX01
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (121 KB)
MSDSNot Available
Pharmacoeconomics
Manufacturers
  • Speciality european pharma ltd
Packagers
Dosage formsNot Available
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5843901 No1995-12-012015-12-01Us
US5968895 No1996-12-112016-12-11Us
US6180608 No1996-12-112016-12-11Us
US6423686 No1995-06-072015-06-07Us
US6699833 No1996-12-112016-12-11Us
Properties
StateLiquid
Experimental PropertiesNot 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
antagonist
General Function:
Peptide binding
Specific Function:
Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This receptor mediates its action by association with G-proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act as an inhibitor of GnRH-R signaling.
Gene Name:
GNRHR
Uniprot ID:
P30968
Molecular Weight:
37730.355 Da
References
  1. Debruyne FM: Gonadotropin-releasing hormone antagonist in the management of prostate cancer. Rev Urol. 2004;6 Suppl 7:S25-32. [PubMed:16985933 ]
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Drug created on June 13, 2005 07:24 / Updated on December 09, 2016 02:38