CYP3A4 inhibition in human liver microsomes by casopitant and GSK525060
| Probe Substrate | IC50 | ||
|---|---|---|---|
| Direct Inhibition | Metabolism-Dependent Inhibition | ||
| μM | fold change | ||
| Casopitant | Midazolam | 9.86 ± 1.78a | 4.27 |
| Nifedipine | 9.72 ± 1.18 | 3.37 | |
| GSK525060 | Midazolam | 8.22 ± 2.76 | 2.96 |
| Nifedipine | 5.60 ± 0.45 | 13.7 | |
↵a S.E. provided by GraFit.