Table 2.

Effects of gefitinib and erlotinib on the disappearance of midazolam and formation of 1-hydroxymidazolam in human liver and intestinal microsomes

Midazolam disappearance rate (% of control)1-Hydroxymidazolam formation rate (% of control)
Liver microsomes (μmol/L)
Intestinal microsomes (μmol/L)
  • NOTE: Values are presented as the mean of duplicate determinations. Midazolam initial concentration was 20 μmol/L. The control was midazolam disappearance rate or 1-hydroxymidazolam formation rate in the absence of an effector (e.g., gefitinib, erlotinib, or imatinib). Imatinib (a reported CYP3A inhibitor) was used as the control experiment.