Effect of inactive microsomal protein concentration on inhibitory effect of CYP3A inhibitors at a constant active protein concentration (0.25 mg/ml)
| Inhibitor (μM) | Mean (± S.E.) Fraction (Rv) of Control (Uninhibited) Diazepam 3-Hydroxylation Velocity at Inactive Protein Concentration | ||||
|---|---|---|---|---|---|
| 0 | 0.25 | 0.75 | 1.75 | 2.75 | |
| mg/ml | |||||
| Ketoconazole (0.05) | 0.38 ± 0.04 | 0.43 ± 0.06 | 0.51 ± 0.05 | 0.56 ± 0.04 | 0.67 ± 0.04 |
| OH-Itraconazole (0.25) | 0.33 ± 0.05 | 0.37 ± 0.06 | 0.43 ± 0.07 | 0.54 ± 0.04 | 0.51 ± 0.03 |
| Fluconazole (10) | 0.42 ± 0.04 | 0.44 ± 0.04 | 0.48 ± 0.05 | 0.47 ± 0.08 | 0.49 ± 0.08 |
Table entries (Rv values) are defined from eq. 1 in text.