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Identification
NameAbarelix
Accession NumberDB00106  (BIOD00051, BTD00051)
Typebiotech
Groupsapproved, investigational, withdrawn
Description

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 structureNo structure small
Protein chemical formulaC72H95ClN14O14
Protein average weight1416.0630
Sequences
SynonymsNot Available
SaltsNot Available
Brand names
NameCompany
PlenaxisPraecis Pharmaceuticals
Brand mixturesNot Available
CategoriesNot Available
CAS number183552-38-7
Taxonomy
KingdomOrganic Compounds
SuperclassOrganic Acids
ClassCarboxylic Acids and Derivatives
SubclassAmino Acids, Peptides, and Analogues
Direct parentPeptides
Alternative parentsNot Available
SubstituentsNot Available
Classification descriptionNot Available
Pharmacology
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%
Metabolism

<i>In vitro</i> hepatocyte (rat, monkey, human) studies and <i>in vivo</i> 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 <i>in vitro</i> or <i>in vivo</i>. 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
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption Not Available Not Available
Blood Brain Barrier Not Available Not Available
Caco-2 permeable Not Available Not Available
P-glycoprotein substrate Not Available Not Available
P-glycoprotein inhibitor I Not Available Not Available
P-glycoprotein inhibitor II Not Available Not Available
Renal organic cation transporter Not Available Not Available
CYP450 2C9 substrate Not Available Not Available
CYP450 2D6 substrate Not Available Not Available
CYP450 3A4 substrate Not Available Not Available
CYP450 1A2 substrate Not Available Not Available
CYP450 2C9 substrate Not Available Not Available
CYP450 2D6 substrate Not Available Not Available
CYP450 2C19 substrate Not Available Not Available
CYP450 3A4 substrate Not Available Not Available
CYP450 inhibitory promiscuity Not Available Not Available
Ames test Not Available Not Available
Carcinogenicity Not Available Not Available
Biodegradation Not Available Not Available
Rat acute toxicity Not Available Not applicable
hERG inhibition (predictor I) Not Available Not Available
hERG inhibition (predictor II) Not Available Not Available
Pharmacoeconomics
Manufacturers
  • Speciality european pharma ltd
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for suspensionIntramuscular
PricesNot Available
Patents
CountryPatent NumberApprovedExpires (estimated)
United States59688951996-12-112016-12-11
United States64236861995-06-072015-06-07
Properties
Stateliquid
Experimental PropertiesNot Available
Spectra
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferenceNot Available
External Links
ResourceLink
PharmGKBPA164754915
IUPHAR1188
Guide to Pharmacology1188
RxListhttp://www.rxlist.com/cgi/generic/plenaxis.htm
Drugs.comhttp://www.drugs.com/cdi/abarelix.html
WikipediaAbarelix
ATC CodesL02BX01
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelshow(121 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
TacrolimusAdditive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
ThiothixeneMay cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
ToremifeneAdditive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
TrimipramineAdditive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
VoriconazoleAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
VorinostatAdditive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
ZiprasidoneAdditive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
ZuclopenthixolAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Zuclopenthixol acetateAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Zuclopenthixol decanoateAdditive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Food InteractionsNot Available

1. Gonadotropin-releasing hormone receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Gonadotropin-releasing hormone receptor P30968 Details

References:

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

Comments
Drug created on June 13, 2005 07:24 / Updated on July 08, 2013 14:15