Steady-state Cmax values of HIV protease inhibitors in comparison to their IC50 values inhibiting hOCT1
| Compounds | Cmax, steady-state | IC50 |
|---|---|---|
| μM | ||
| Indinavir | 12.6 ± 42-a | 61.7 ± 18.4 |
| Nelfinavir | 4.5–6.02-b | 21.8 ± 5.4 |
| Ritonavir | 15.52-c | 5.18 ± 1.21 |
| Saquinavir | 2–42-d | 8.26 ± 1.64 |
↵2-a 800 mg three times daily (n = 16) (Crixivan package insert)
↵2-b 750 mg three times daily (data listed were converted from 3 to 4 μg/ml using molecular weight of 664 g/mol) (Viracept package insert)
↵2-c 600 mg 12 hourly (number listed was converted from 11.2 μg/ml using molecular weight of 721 g/mol) (Norvir package insert)
↵2-d 600 mg 1200 mg ID) [data listed were converted from 1420 ng/ml (for patient) and 2477 ng/ml (for health volunteer) using molecular weight of 671 g/mol] (Fortovase package insert)