clopidogrel active metabolite

R-130964 is the active thiol metabolite of clopidogrel, a thienopyridine prodrug and oral antiplatelet agent. It is generated in the liver via a two-step cytochrome P450-mediated oxidative process following clopidogrel administration. R-130964 irreversibly binds to the P2Y12 purinergic receptor on platelet surfaces, specifically to the cysteine residue (Cys97) in the receptor, which permanently blocks ADP-dependent platelet activation and aggregation for the lifespan of the platelet. Only about 5–10% of ingested clopidogrel is converted to R-130964 due to competing hepatic esterase metabolism, and genetic variability in CYP isoenzymes (notably CYP2C19) influences exposure to and activity of R-130964. The metabolite's formation and subsequent action underpin the antithrombotic clinical efficacy of clopidogrel in cardiovascular diseases[2][1].

Other names

clopidogrel active metaboliteR-130964R130964R 130964