Inactivation kinetic values for mechanism-based inactivators of human P450 enzymes
Inactivator | P450 | kinact | KI | kinact/KI |
|---|---|---|---|---|
| min-1 | μM | ml/min/μmol | ||
| Furafylline | CYP1A2 | 0.19 | 1.6 | 120 |
| Zileuton | CYP1A2 | 0.11 | 89 | 1.2 |
| PPP | CYP2B6 | 0.10 | 5.3 | 19 |
| thioTEPA | CYP2B6 | 0.17 | 5.3 | 32 |
| CYP2C8 | 0.026 | 88 | 0.30 | |
| CYP2C19 | 0.029 | 1100 | 0.026 | |
| CYP3A (midazolam) | 0.035 | 300 | 0.12 | |
| CYP3A (testosterone) | 0.033 | 220 | 0.15 | |
| Desethylamiodarone | CYP2B6 | 0.026 | 14 | 1.9 |
| CYP2C8 | 0.009 | 4.4 | 2.1 | |
| CYP2C9 | 0.053 | 38 | 1.4 | |
| CYP2D6 | 0.029 | 24 | 1.2 | |
| CYP3A (midazolam) | 0.012 | 2.8 | 4.3 | |
| CYP3A (testosterone) | 0.018 | 4.0 | 4.5 | |
| Tienilic acid | CYP2C9 | 0.28 | 1.0 | 280 |
| Ticlopidine | CYP1A2 | 0.011 | 5.2 | 2.1 |
| CYP2B6 | 0.30 | 0.57 | 530 | |
| CYP2C19 | 0.097 | 4.3 | 23 | |
| CYP3A (midazolam) | 0.039 | 77 | 0.51 | |
| CYP3A (testosterone) | 0.019 | 210 | 0.090 | |
| MDMA | CYP1A2 | 0.014 | 180 | 0.078 |
| CYP2D6 | 0.38 | 6.3 | 60 | |
| Paroxetine | CYP2D6 | 0.17 | 0.81 | 210 |
| CYP3A (midazolam) | 0.011 | 13 | 0.85 | |
| CYP3A (testosterone) | 0.014 | 23 | 0.64 | |
| Diltiazem | CYP3A (midazolam) | 0.012 | 4.5 | 2.7 |
| CYP3A (testosterone) | 0.015 | 2.4 | 6.3 | |
| Erythromycin | CYP3A (midazolam) | 0.036 | 10 | 3.6 |
| CYP3A (testosterone) | 0.039 | 9.8 | 4.0 | |
| Ritonavir | CYP3A (midazolam) | 0.45 | 0.38 | 1200 |
| CYP3A (testosterone) | 0.28 | 0.18 | 1500 | |
| Verapamil | CYP3A (midazolam) | 0.043 | 1.8 | 24 |
|
| CYP3A (testosterone) | 0.043 | 1.7 | 25 |