Table 2.
Effect of CMV423 and rac-RPR127025 on in vitro indinavir oxidation and AZT glucuronidation. Experiments were performed as described in Methods. Values are mean of duplicate assays. CVs were below 6%.
| Substrate (µm) | Inhibitor (10 µm) | Design | Effect on substrate biotransformation (%) |
|---|---|---|---|
| Indinavir 0.1 | CMV423 | Co-incubation | −3 |
| Pre-incubation | −2 | ||
| Indinavir 1 | CMV423 | Co-incubation | −24 |
| Pre-incubation | +2 | ||
| Indinavir 1 | rac-RPR 127025 | Co-incubation | 0 |
| Pre-incubation | +12 | ||
| AZT 250 | CMV423 | Co-incubation | 0 |
| AZT 1000 | CMV423 | Co-incubation | −11 |