Effect of P450 inhibitors on amprenavir metabolism by adult human liver microsomes
| M1 | M2 | M3 | M4 | M5 | Total | |
|---|---|---|---|---|---|---|
| Liver 1 control | 100% | 100% | 100% | 100% | 100% | 100% |
| Sulfaphenazole (2C9), 30 μM | 92 | 81 | 100 | 37 | 126 | 93 |
| Quinidine (2D6), 10 μM | 160 | 72 | 35 | 87 | 106 | 86 |
| Ketoconazole (3A4/5), 10 μM | 112 | 0 | 0 | 125 | 83 | 39 |
| Ritonavir (3A4), 3.7 μM | 20 | 6 | 16 | 62 | 10 | 13.5 |
| Liver 3 control | 100% | 100% | 100% | 100% | ||
| Sulfaphenazole (2C9), 30 μM | 88 | 108 | 117 | 104 | ||
| Quinidine (2D6), 10 μM | 125 | 112 | 100 | 112 | ||
| Ketoconazole (3A4/5), 10 μM | 38 | 56 | 11 | 41 | ||
| Ritonavir (3A4), 3.7 μM | 0 | 2 | 0 | 1 |
Values represent the residual activity expressed as a percentage of the control activity in two different incubations performed on two separate livers.