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1664 details
Primary information
ThPP IDTh1156
Therapeutic Peptide/Protein NameAbarelix
SequenceN.A. view full sequnce in fasta
Functional ClassificationIIIc
Molecular Weight1416.063
Chemical FormulaC72H95ClN14O14
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life13.2 ± 3.2 days
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.
Indication/DiseaseFor 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
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.
MetabolismIn 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.
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 DistributionN.A.
ClearanceN.A.
CategoriesAnti-Testosterone Agents
Patents NumberUS5968895
Date of Issue11/12/96
Date of Expiry11/12/13
Drug InteractionTacrolimus, Thiothixene, Toremifene, Trimipramine, Voriconazole, Vorinostat, Ziprasidone, Zuclopenthixol- All above drugs cause Additive QTc Prolongation and increases the risk of severe ventricular arrythmias
TargetGonadotropin-releasing hormone receptor
Information of corresponding available drug in the market
Brand NamePlenaxis
CompanySpeciality european pharma
Brand DiscriptionPlenaxis is a synthetic decapeptide with potent antagonistic activity against naturally occurring gonadotropin releasing-hormone (GnRH). Plenaxis inhibits gonadotropin and related androgen production by directly and competitively blocking GnRH receptors in the pituitary.
Prescribed forPlenaxis is indicated for the palliative treatment of men with advanced symptomatic prostate cancer, in whom LHRH agonist therapy is not appropriate and who refuse surgical castration, and have one or more of the following: (1) risk of neurological compromise due to metastases, (2) ureteral or bladder outlet obstruction due to local encroachment or metastatic disease, or (3) severe bone pain from skeletal metastases persisting on narcotic analgesia.
Chemical NameAbarelix is chemically described as acetyl-D-β-naphthylalanyl-D-4-chlorophenylalanyl- D-3-pyridylalanyl-L-seryl-L-N-methyl-tyrosyl-D-asparagyl-L-leucyl-L-N(ε)-isopropyllysyl- L-prolyl-D-alanyl-amide.
FormulationThe single-dose vial contains 113 mg of anhydrous free base abarelix peptide (net) supplied in an abarelix CMC complex. This complex also contains 19.1 to 31 mg of CMC. After the vial is reconstituted with 2.2 mL of 0.9% sodium chloride injection
Physcial AppearnceAbarelix for injectable suspension is supplied as a white to off-white sterile dry powder
Route of AdministrationIntramuscular Injection
Recommended Dosage The recommended dose of Plenaxis is 100 mg administered intramuscularly to the buttock on Day 1, 15, 29 (week 4) and every 4 weeks thereafter.
ContraindicationPlenaxis is not indicated in women or pediatric patients. In addition, Plenaxis may cause fetal harm if administered to a pregnant woman.
Side Effects Diarrhea, Dizziness, Flushing of Skin, Headache, Constipation, Sleep Disturbance
Useful Linkhttp://www.rxlist.com/plenaxis-drug.htm
PubMed ID21904569
3-D StructureN.A.