Kinetic parameters for cDNA expressed CYP3A4 and CYP3A5 in the presence of ketoconazole or fluconazole2-a
| Inhibitor | Inhibition Type | Vmax | Km | Ki |
|---|---|---|---|---|
| pmol/min/pmol | μM | |||
| Ketoconazole | ||||
| CYP3A4 | Noncompetitive | 5.57 ± 0.661 | 3.13 ± 0.194 | 26.7 ± 1.71 nM |
| CYP3A5 | Noncompetitive | 4.62 ± 0.568 | 4.64 ± 1.15 | 109 ± 19.7 nM |
| Fluconazole | ||||
| CYP3A4 | Noncompetitive | 3.87 ± 0.137 | 2.36 ± 0.215 | 9.21 ± 0.51 μM |
| CYP3A5 | Noncompetitive | 4.76 ± 0.423 | 4.13 ± 0.739 | 84.6 ± 12.9 μM |
↵2-a For each inhibitor parameter estimates (± asymptotic S.E.) were obtained from a nonlinear regression fit of the complete data set.