TABLE 3

Inhibition of human liver CYPs by fungal CYP51 inhibitors

InhibitorIC50 (μM)a
CYP2C9CYP2C19CYP3A4bCYP3A4c
Clotrimazole1.4 (0.1)0.6 (0.2)0.03 (0.01)0.045 (0.001)
Fluconazole34 (10)13 (9)32 (5)6 (2)
Itraconazole80 (28)78 (31)0.08 (0.02)0.13 (0.06)
Voriconazole10 (5)10 (4)13 (4)3.8 (0.2)
VT-112987 (21)110 (80)79 (23)178 (31)
  • a Values are averages of 2 to 4 separate determinations, and standard deviations are provided in parentheses.

  • b Testosterone as the substrate.

  • c Midazolam as the substrate.