Table 4.
Concentration-dependent effects of cimetidine, enoxacine and imipramine on CMV423 metabolism by human liver microsomes following co-incubation. The results are expressed as a percentage of controls (vehicles only). Each value represents the mean % change calculated from duplicate experiments. Coefficients of variation were below 15%.
| Drug | Concentration (µm) | Effect on RPR 127025 formation (%) | Effect on RPR 123830 formation (%) |
|---|---|---|---|
| Cimetidine | 3 | 0.0 | + 2 |
| 10 | −6.0 | + 10 | |
| 30 | −6.0 | + 19 | |
| 100 | −12.0 | + 5 | |
| 300 | −16.0 | −20 | |
| Enoxacine | 3 | −4.0 | + 7 |
| 10 | −5.0 | 0 | |
| 30 | −12.0 | + 1 | |
| 100 | −24.0 | −25 | |
| 300 | −36.0 | −31 | |
| Imipramine | 0.3 | + 3.0 | −1 |
| 1 | −2.0 | −6 | |
| 3 | −7.0 | −7 | |
| 10 | + 2.0 | −7 | |
| 30 | −12.0 | −10 | |
| 100 | −25.0 | −29 |