Title : Comparison of mechanism-based inhibition of human cytochrome P450 2C19 by ticlopidine, clopidogrel, and prasugrel.

Pub. Date : 2009 Nov

PMID : 19845434






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1 Comparison of mechanism-based inhibition of human cytochrome P450 2C19 by ticlopidine, clopidogrel, and prasugrel. Ticlopidine cytochrome P450 family 2 subfamily C member 19 Homo sapiens
2 Mechanism-based inhibition of CYP2C19 in human liver microsomes by the thienopyridine antiplatelet agents clopidogrel, prasugrel and their thiolactone metabolites was investigated by determining the time- and concentration-dependent inhibition of the activity of S-mephenytoin 4"-hydroxylase as typical CYP2C19 activity and compared with ticlopidine and its metabolite. Ticlopidine cytochrome P450 family 2 subfamily C member 19 Homo sapiens
3 Clopidogrel was shown to be a mechanism-based inhibitor of CYP2C19 with the inactivation kinetic parameters, k(inact) and K(I), equal to 0.0557 min(-1) and 14.3 microM, respectively, as well as ticlopidine (0.0739 min(-1) and 3.32 microM, respectively). Ticlopidine cytochrome P450 family 2 subfamily C member 19 Homo sapiens
4 The thiolactone metabolite of ticlopidine and clopidogrel inhibited CYP2C19 only in a concentration-dependent manner. Ticlopidine cytochrome P450 family 2 subfamily C member 19 Homo sapiens