Effect of isoform-selective CYP inhibitors on the metabolism of ABT-378 by human liver microsomes
| Inhibitor | Percentage of Control Activity | |||
|---|---|---|---|---|
| ABT-378 | M-1 | M-3 | M-4 | |
| Furafylline4-a (5 μM) | 82.2 | 92.3 | 88.6 | 125.7 |
| Coumarin (100 μM) | 111.2 | 115.7 | 95.1 | 117.2 |
| Sulfaphenazole (1 μM) | 111.3 | 166.1 | 96.4 | 122.3 |
| Tranylcypromine (50 μM) | 96.3 | 104.8 | 72.2 | 108.2 |
| Quinidine (1 μM) | 115.5 | 184.4 | 59.3 | 127.9 |
| 4-Methylpyrazole (20 μM) | 112.2 | 174.7 | 82.4 | 123.2 |
| Ketoconazole (1 μM) | 19.6 | 24.7 | 19.1 | 20.8 |
| Troleandomycin4-a (200 μM) | 15.7 | 19.6 | 10.2 | 22.4 |
| Ritonavir (0.1 μM) | 22.1 | 45.7 | 15.7 | 15.6 |
↵4-a Preincubation with NADPH.