TABLE 3.
Inhibition of human liver CYPs by fungal CYP51 inhibitors
| Inhibitor | IC50 (μM)a |
|||
|---|---|---|---|---|
| CYP2C9 | CYP2C19 | CYP3A4b | CYP3A4c | |
| Clotrimazole | 1.4 (0.1) | 0.6 (0.2) | 0.03 (0.01) | 0.045 (0.001) |
| Fluconazole | 34 (10) | 13 (9) | 32 (5) | 6 (2) |
| Itraconazole | 80 (28) | 78 (31) | 0.08 (0.02) | 0.13 (0.06) |
| Voriconazole | 10 (5) | 10 (4) | 13 (4) | 3.8 (0.2) |
| VT-1129 | 87 (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.