TABLE 1

Summary of the KI, kinact, and partition ratios for the mechanism-based inactivation of CYP2B6 WT and C475S

Details for the measurements of the kinetic parameters and partition ratios are under Materials and Methods. The reported data were averaged from four separate experiments.

CYP2B6Clopidogrel2-Oxo-clopidogrel
KIkinactkinact/KIPart. RatioKIkinactkinact/KIPart. Ratio
μMmin1μMmin1
WT2.4 ± 0.330.17 ± 0.0310.07119 ± 46.3 ± 0.720.092 ± 0.0150.01551 ± 8
C475S4.2 ± 0.210.12 ± 0.0150.02917 ± 2N.D.
  • N.D., not determined because of lack of inactivation.