Effect of selective AKR inhibitors on the formation of M28 from boceprevir (20 μM) using pooled human liver cytosol (1.6 mg/ml, 1 h of incubation)
| Inhibitors | Concentrationa | % of Inhibition (IC50) |
|---|---|---|
| μM | ||
| Diazepam | 100 | 75.1 |
| Ibuprofen | 1000 | 70.0 (411.8 μM) |
| Diflunisal | 200 | 89.4 (4.58 μM) |
| Ketoconazole | 2 | 0 |
| Ritonavir (coincubation/preincubation) | 2 | 0 |
↵a Concentrations were based on published literature. Average of duplicate determinations. Coefficient of variation <10%.