|Accession Number||DB00106 (BTD00051, BIOD00051)|
|Groups||Approved, Investigational, Withdrawn|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 chemical formula||C72H95ClN14O14|
|Protein average weight||1416.063 Da|
|External IDs||Not Available|
|Product Ingredients||Not Available|
|Approved Prescription Products||Not Available|
|Approved Generic Prescription Products||Not Available|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|Brand mixtures||Not Available|
For palliative treatment of advanced prostate cancer.
|Structured Indications||Not Available|
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.
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|
13.2 ± 3.2 days
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.
|Pharmacogenomic Effects/ADRs||Not Available|
|Drug Interactions||Not Available|
|Food Interactions||Not Available|
|Synthesis Reference||Not Available|
|General References||Not Available|
|ATC Codes||L02BX01 — Abarelix|
|PDB Entries||Not Available|
|FDA label||Download (121 KB)|
|Dosage forms||Not Available|
|Experimental Properties||Not Available|
|Super Class||Organic Acids|
|Class||Carboxylic Acids and Derivatives|
|Sub Class||Amino Acids, Peptides, and Analogues|
|Alternative Parents||Not Available|
|Molecular Framework||Not Available|
|External Descriptors||Not Available|
- Pharmacological action
- 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:
- Uniprot ID:
- Uniprot Name:
- Gonadotropin-releasing hormone receptor
- Molecular Weight:
- 37730.355 Da
- Debruyne FM: Gonadotropin-releasing hormone antagonist in the management of prostate cancer. Rev Urol. 2004;6 Suppl 7:S25-32. [PubMed:16985933 ]