General Information about Clopidogrel Bisulfate
Clopidogrel bisulfate is a prodrug, meaning it is dispensed as an inactive precursor and must be converted by the body to its active form. It is absorbed in the intestines and converted to its active metabolite in the liver by cytochrome P450 enzymes by two sequential oxidative steps. The active metabolite can then go on to bind the P2Y’12 receptor on the surface of platelet cells, inhibiting ADP from binding. When ADP-mediated activation of the glycoprotein GPIIb/IIIa complex is blocked, platelet aggregation that contributes to blood clots is inhibited.
Clopidogrel bisulfate became FDA approved as an inhibitor of platelet aggregation in patients with acute coronary syndrome (ACS) under the trade name Plavix in 1997. It is currently manufactured through large-scale synthetic organic chemistry methods starting from simple, commercially available precursors.