Kinetics of inhibition of microsomal metabolism of representative drugs
Results are expressed as estimate (± S.E.).
| CYP3A Substrate | Modifier | Ki (μM) | Km (μM) | Vmax |
|---|---|---|---|---|
| nmol min−1 mgHLM−1 | ||||
| Midazolam | KTZ | 0.007 (0.002) | 1.7 (0.6) | 2.6 (0.3) |
| PPI-2458 | 58 (7) | 1.9 (0.3) | 2.6 (0.1) | |
| Nifedipine | KTZ | 0.011 (0.001) | 74 (11) | 2.1 (0.2) |
| PPI-2458 | 403 (101) | 87 (20) | 2.2 (0.3) | |
| Testosterone | KTZ | 0.049 (0.007) | 145 (48) | 5.8 (1.4) |
| PPI-2458 | 287 (48) | 131 (25) | 5.4 (0.8) |