130209-90-4

Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y₁₂ receptor (IC₅₀ = 100 nM).^1,2 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.³ 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.⁴

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1. Savi, P., Labouret, C., Delesque, N., et al. P2Y12, a new platelet ADP receptor, target of clopidogrel Biochem. Bioph. Res. Commun. 283(2),379-383(2001).
2. von Kügelgen, I. Pharmacological profiles of cloned mammalian P2Y-receptor subtypes Pharmacol. Ther. 110(3),415-432(2006).
3. Quinn, M.J., and Fitzgerald, D.J. Ticlopidine and clopidogrel Circulation 100(15),1667-1672(1999).
4. Angiolillo, D.J., Fernandez-Ortiz, A., Bernardo, E., et al. Variability in individual responsiveness to clopidogrel: Clinical implications, management, and future perspectives J. Am. Coll. Cardiol. 49(14),1505-1516(2007).