Hepatocyte kinetic parameters for uptake and metabolism of saquinavir, ritonavir, and nelfinavir (n = 3) Mean ± S.D. of triplicate in vitro preparations.
Metabolism Parameters | Uptake Parameters | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Km | Vmax | Clint | Km | Vmax | Perm | |||||
| μM | pmol/min/106 cells | μl/min/106 cells | μM | nmol/min/106 cells | μl/min/106 cells | |||||
| Saquinavir | 0.27 ± 0.15 | 114 ± 62.5 | 486 ± 256 | >28 | >18 | 520 | ||||
| Ritonavir | 0.034 ± 0.013 | 21.6 ± 6.18 | 734 ± 384 | 14 ± 5.4 | 15 ± 6 | 1070 | ||||
| Nelfinavir | 0.21 ± 0.12 | 232 ± 50.2 | 1290 ± 464 | 22.4 ± 5 | 58.4 ± 17.8 | 2670 | ||||