Drug nameAbarelix
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.
DrugBankPrimary Accession Number: DB00106
DINNot available
TypeApproved, Biotech, Investigational, Withdrawn
IndicationFor palliative treatment of advanced prostate cancer.
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.
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.
Protein Binding96-99%
Interactions
RXListhttp://www.rxlist.com/cgi/generic/plenaxis.htm
KEGGdrug: D02738 / compound: Not Available
PubChemcompound: 16131215 / substance: 12015126
PharmGKBPA164754915
Metabolizing Enzymes
NameGeneEntrezIDUniprotSNP
Target
NameGeneEntrezIDSwissprotSNP
Gonadotropin-releasing hormone receptorGNRHR2798GNRHR_HUMANrs35400155 rs28933074 rs13149772 rs13130501 rs4986942
FilesDB00106.mol | DB00106_2003-12-01.pdf | pdb_652907351309-0.pdb | sdf_8914727314996-0.sdf |
Smilesisomeric:
CC(C)C[C@H](NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CC1=CC=C(O)C=C1)N(C)C(=O)
[C@H](CO)NC(=O)[C@@H](CC1=CN=CC=C1)NC(=O)[C@@H](CC1=CC=C(Cl)C=C1)NC(=O
)[C@@H](CC1=CC2=C(C=CC=C2)C=C1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1
CCC[C@H]1C(=O)N[C@H](C)C(N)=O
canonical:
CC(C)CC(NC(=O)C(CC(N)=O)NC(=O)C(CC1=CC=C(O)C=C1)N(C)C(=O)C(CO)NC(=O)C(
CC1=CN=CC=C1)NC(=O)C(CC1=CC=C(Cl)C=C1)NC(=O)C(CC1=CC2=C(C=CC=C2)C=C1)N
C(C)=O)C(=O)NC(CCCCNC(C)C)C(=O)N1CCCC1C(=O)NC(C)C(N)=O

© 2010-2020 All rights reserved. King Abdullah University of Science and Technology, All rights reserved