Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation^[1]. IC50 & Target: P2Y12 receptor^[1] In Vivo: In rat platelets, Prasugrel active metabolite inhibits in vitro platelet aggregation induced by adenosine ADP (10μM) with an IC₅₀ value of 1.8 μM^[2].
Prasugrel acts faster and is significantly more potent than Clopidogrel in vivo. Prasugrel is an inactive prodrug that requires metabolic processing in vivo to generate the active antiplatelet metabolite. Prasugrel is rapidly absorbed from the gut. After oral administration of standard-loading doses of 60 mg, maximum plasma levels of the active metabolite are achieved within 1 h, effective, maximum inhibition of platelet aggregation at 1-2 h^[1].