Effects of isoform-selective inhibitors of human P450 isoforms on the metabolism of lasofoxifene by human liver microsomes
Inhibitor | Concentration | Inhibited P450 Isoforms | Percentage Inhibition | ||
|---|---|---|---|---|---|
| 7-Hydroxy-lasofoxifene | 5-Hydroxy-lasofoxifene | ||||
| μM | |||||
| Control | 0.0 | 0.0 | |||
| Furafylline | 40 | CYP1A1/1A2 | 45.4 | 14.9 | |
| Quercetin | 40 | CYP2C8 | 60.5 | 22.5 | |
| Sulfaphenazole | 40 | CYP2C9/2C19 | 37.8 | 3.10 | |
| Quinidine | 1 | CYP2D6 | 61.3 | 10.2 | |
| Ketoconazole | 1 | CYP3A4 | 100 | 82.6 | |
| ABT | 100 | P450 | 100 | 100 | |