Prasugrel

Prasugrel, a thienopyridine derivative, is a platelet activation and aggregation inhibitor structurally and pharmacologically related to clopidogrel and ticlopidine. Similar to clopidogrel, prasugrel is a prodrug that requires enzymatic transformation in the liver to its active metabolite, R-138727. R-138727 irreversibly binds to P2Y12 type ADP receptors on platelets thus preventing activation of the GPIIb/IIIa receptor complex. As a result, inhibition of ADP-mediated platelet activation and aggregation occurs. Prasugrel was developed by Daiichi Sankyo Co. and is currently marketed in the United States and Canada in cooperation with Eli Lilly and Company for acute coronary syndromes planned for percutaneous coronary intervention (PCI) . FDA approved in 2009. (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.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.