A prodrug of the platelet purinergic P2Y12 receptor antagonist
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Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). Clopidogrel inhibits ADP-induced platelet aggregation ex vivo and functions as a prodrug whereupon biotransformation to its active metabolite via CYP2C19 in the liver enables its anti-aggregating activity. Marketed under the name Plavix?, clopidogrel in combination with aspirin has been shown to be beneficial in the prevention of vascular ischemic events for patients without deficiencies in CYP2C19-related metabolism.
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