Inactivation of CYP3A4 in human hepatocytes using three different TDI methods
| Inhibitor and Concentration | Percentage Inhibition of CYP3A4 Activity after 1 h Preincubation | ||
|---|---|---|---|
| Wash Method | Add Method | Dilution Method | |
| Verapamil | |||
| 3 μM | 57.0 | 51.0 | 55.0 |
| 10 μM | 71.6 | 74.0 | 70.1 |
| 30 μM | 72.4 | 77.2 | 73.9 |
| Erythromycin | |||
| 3 μM | 15.6 | 6.4 | 9.0 |
| 10 μM | 41.0 | 27.5 | 30.0 |
| 30 μM | 66.2 | 65.5 | 69.1 |
| TAO | |||
| 0.1 μM | 5.6 | 11.2 | 8.3 |
| 1 μM | 29.4 | 44.0 | 38.0 |
| 10 μM | 57.5 | 75.5 | 80.0 |