Kinetic Parameters (% coefficient of variation) for enzyme inactivation
| Protease Inhibitor | kinact | KI | kinact/KI |
|---|---|---|---|
| min-1 | μM | min-1 × nM-1 | |
| Human Liver Microsomes | |||
| Ritonavir | 0.40 (21) | 0.17 (38) | 2353 |
| Amprenavir | 0.59 (75) | 0.37 (24) | 1595 |
| Lopinavir | 0.11 (9.3) | 1.00 (25) | 110 |
| Saquinavir | 0.26 (5.1) | 0.65 (17) | 400 |
| Nelfinavir | 0.22 (7.1) | 1.00 (27) | 220 |
| Indinavir | — | — | — |
| CYP3A4(+b5) | |||
| Ritonavir | 0.32 (7.5) | 0.10 (20) | 3200 |
| Amprenavir | 0.73 (9.1) | 0.26 (18) | 2808 |
| Lopinavir | 0.10 (4.3) | 0.41 (14) | 244 |
| Saquinavir | 0.31 (6.8) | 0.17 (25) | 1824 |
| Nelfinavir | 0.22 (8.5) | 0.48 (30) | 458 |
| Indinavir | — | — | — |
| CYP3A5 | |||
| Ritonavir | 0.08 (15) | 0.12 (39) | 667 |
| Amprenavir | 0.35 (5.7) | 0.20 (27) | 1750 |
| Lopinavir | 0.05 (6.5) | 1.00 (27) | 50 |
| Saquinavir | — | — | — |
| Nelfinavir | 0.47 (4.5) | 0.57 (20) | 825 |
| Indinavir | — | — | — |
—, parameters not estimated; no inactivation detected.