|Accession Number||DB00106 (BIOD00051, BTD00051)|
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 chemical formula||C72H95ClN14O14|
|Protein average weight||1416.0630|
|Brand mixtures||Not Available|
|Indication||For palliative treatment of advanced prostate cancer.|
|Pharmacodynamics||Used 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 action||Abarelix binds to the gonadotropin releasing hormone receptor and acts as a potent inhibitor of gonadotropin secretion.|
|Absorption||Following 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 distribution||Not Available|
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 elimination||Not Available|
|Half life||13.2 ± 3.2 days|
|Toxicity||The 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.|
|Experimental Properties||Not Available|
|Synthesis Reference||Not Available|
|General Reference||Not Available|
|PDB Entries||Not Available|
|FDA label||show (121 KB)|
|Food Interactions||Not Available|
Receptor for gonadotropin releasing hormone (GnRH) that mediate the action of GnRH to stimulate the secretion of the gonadotropic hormones (LH and FSH). This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Isoform 2 may act a an inhibitor of GnRH-R signalingOrganism class: human
UniProt ID: P30968
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report
Searched, but no enzymes found.
Searched, but no transporters found.
Searched, but no carriers found.