Fig. 1: Mechanism of action of clopidogrel. | npj Genomic Medicine

Fig. 1: Mechanism of action of clopidogrel.

From: A narrative review of research advancements in pharmacogenetics of cardiovascular disease and impact on clinical implications

Fig. 1

The intestinal absorption of clopidogrel is restricted by P-glycoprotein (P-gp), which is encoded by ABCB1. Carboxylesterase 1 (CES1) hydrolyses 85% of its uptake into inactive metabolites. Only 15% of inactive clopidogrel is oxidised by liver-resident cytochrome P450 (CYP450) enzymes to 2-oxo-clopidogrel, which is also inactive. Subsequently, CYP450 and paraoxonase enzymes convert 2-oxo-clopidogrel into active metabolites (thiols), which bind to the P2Y12 receptor on the platelet surface. This binding prevents the activation of the GPIIb/IIIa complex by ADP, which inhibits platelet activation (modified from refs. 6,7). Figure created with Bio Render.com.

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