TABLE 2

Enzyme kinetic parameters of the formation of the pharmacologically active metabolite of clopidogrel from 2-oxo-clopidogrel

The assays were performed by using the microsomes baculovirus/insect cells expressing human cytochrome P450 (Supersomes). Km and Vmax values were expressed as mean ± S.E. of parameter estimate. CLint and fmP450 (P450 contribution ratio) values were scaled to eqs. 2 and 3 under Materials and Methods to determine contribution.

Incubation TimeKmVmaxVmax/KmEnzyme Abundances*CLint, expressed P450fmP450 %
minμMpmol/pmol P450/minμl/pmol P450/minpmol P450/mg proteinμl/mg protein/min
CYP2B6151.62 ± 0.082.48 ± 0.031.531116.832.9
CYP2C93018.1 ± 3.80.855 ± 0.0840.0472733.456.76
CYP2C191512.1 ± 2.29.06 ± 0.680.7491410.520.6
CYP3A41527.8 ± 4.23.63 ± 0.290.13115520.339.8
  • * The abundances of CYP3A4, CYP2B6, CYP2C19, and CYP2C9 were obtained from the reported data in Rowland Yeo et al. (2004).