The effects of chemical inhibitors on the in vitro rates of NVP metabolite formation by human hepatic microsomes and cDNA-expressed CYP in incubations with 100 μM NVP
| Inhibitor | NVP Metabolite | ||||||
|---|---|---|---|---|---|---|---|
| 2-HydroxyNVP | 3-HydroxyNVP | 8-HydroxyNVP | 12-HydroxyNVP | ||||
| HHM4-a | CYP3A4 | HHM | CYP2B6 | HHM | HHM | CYP3A4 | |
| Ketoconazole (0.5 μM) | 724-b | 83 | 31 | 25 | NA | 56 | 78 |
| Ketoconazole (2.5 μM) | 90 | 95 | 47 | 56 | NA | 71 | 92 |
| Troleandomycin (50 μM) | 89 | 100 | 25 | 0 | NA | 70 | 100 |
| Erythromycin (50 μM) | 60 | NA4-c | 0 | 0 | NA | 50 | NA |
| Quinidine (15 μM) | 3 | NA | 0 | NA | 7 | 0 | NA |