IC50 values of inhibitors from human hepatocytes suspended in human plasma: single IC50 assessment (20-min inhibitor incubation alone) and independent multiple IC50 assessment (0-, 10-, and 20-min inhibitor incubation alone)
Each number represents the mean ± S.E. of estimate of triplicate determinations.
| Inhibitor | Single IC50 Assessment 20 Min | Multiple IC50 Assessment | ||
|---|---|---|---|---|
| 0 Min | 10 Min | 20 Min | ||
| μM | ||||
| Ketoconazole | 1.26 ± 0.23 | 0.98 ± 0.14 | 1.08 ± 0.11 | 1.14 ± 0.21 |
| Fluconazole | 7.61 ± 2.67 | 7.05 ± 1.83 | 8.05 ± 1.78 | 7.57 ± 2.34 |
| Aprepitant | 24.10 ± 7.30 | 35.62 ± 8.30 | 38.10 ± 10.40 | 23.09 ± 6.80 |
| Voriconazole | 3.01 ± 0.58 | 3.82 ± 0.73 | 4.20 ± 0.39 | 3.32 ± 0.64 |
| Nefazodone | 1.70 ± 0.31 | 27.21 ± 9.15 | 4.75 ± 0.93 | 1.59 ± 0.23 |
| Troleandomycin | 0.16 ± 0.02 | 3.48 ± 0.49 | 0.54 ± 0.11 | 0.23 ± 0.03 |
| Erythromycin | 2.64 ± 0.93 | 12.73 ± 3.02 | 4.79 ± 0.89 | 2.58 ± 0.82 |
| Clarithromycin | 1.98 ± 0.60 | 16.24 ± 4.11 | 2.55 ± 1.33 | 1.68 ± 0.47 |
| Diltiazem | 1.94 ± 0.24 | 3.83 ± 0.88 | 2.22 ± 0.73 | 2.28 ± 0.99 |
| Saquinavir | 4.57 ± 0.52 | 5.56 ± 1.06 | 7.09 ± 3.26 | 3.83 ± 0.64 |
| Itraconazole | 0.22 ± 0.05 | 0.78 ± 0.12 | 1.22 ± 0.15 | 0.37 ± 0.06 |
| Conivaptan | 1.70 ± 0.56 | 46.11 ± 15.97 | 2.69 ± 0.67 | 1.53 ± 0.17 |
| Ritonavir | 0.15 ± 0.01 | 0.16 ± 0.01 | 0.13 ± 0.01 | 0.13 ± 0.01 |