Effect of fluvastatin on the metabolism of characteristic cytochrome P-450 substrates and potentially coadministered compounds (IC50) in human liver microsomes
| Substrate | IC50 | Ki | Pathway | Enzyme |
|---|---|---|---|---|
| μM | μM | |||
| Phenacetin | >100 | O-Deethylation | CYP1A2 | |
| Paclitaxel | 20 | 6α-Hydroxylation | CYP2C8 | |
| Tolbutamide | 0.3 ± 0.1 | 4-Hydroxylation | CYP2C9 | |
| Diclofenac | 0.5 ± 0.1 | 4-Hydroxylation | CYP2C9 | |
| (S)-Mephenytoin | >100 | 4-Hydroxylation | CYP2C19 | |
| Cyclosporine A | >100 | Hydroxylation | CYP3A | |
| N-Demethylation | ||||
| Glibornuride | 9.4 ± 2.1 | |||
| Glyburide | 5.9 ± 0.8 | Cyclohexyl hydroxylation |