P450 inhibition by laromustine: estimates of [I]/Ki based on various clinical estimates of plasma Cmax
P450 Enzyme | Ki Value (in Vitro) | [I]/Ki | ||||
|---|---|---|---|---|---|---|
| Minimum Cmaxa | Average Cmaxa | Maximum Cmaxa | ||||
| μM | ||||||
| CYP2B6 | 125 | 0.010 | 0.200 | 1.02 | ||
| CYP2C19 | 349 | 0.003 | 0.072 | 0.367 | ||
| CYP3A4/5 | 297 | 0.004 | 0.084 | 0.431 | ||
↵ a Values of [I] are from the lowest plasma Cmax (1.2 μM), the average plasma Cmax (25 μM), and the highest plasma Cmax, (128 μM) after a 600 mg/m2 i.v. dose of laromustine in two clinical studies (Vion studies CLI-033b and CLI-043b).