The FDA has approved prasugrel (Effient – Lilly/Daiichi Sankyo), an oral antiplatelet drug, for use with aspirin to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndromes (ACS) being managed with percutaneous coronary intervention (PCI).1 It will compete with clopidogrel (Plavix) for such use.2,3

PHARMACOLOGY — Prasugrel is a thienopyridine prodrug that must undergo hydrolysis by intestinal esterases and oxidation by CYP3A4 and CYP2B6 to be converted to its active metabolite. The active metabolite binds to the P2Y12 adenosine diphosphate (ADP) receptor on the surface of platelets, leading to irreversible inhibition of platelet activity for the 7-10 day lifespan of the platelet. Genetic reducedfunction polymorphisms, which may interfere with conversion of clopidogrel by CYP2C19 to its active form in as many as 30% of ... more      

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