Enzyme kinetic constants for glucuronide formation of various antifungal agents in recombinant enzyme UGT1A4 except for fluconazole for which UGT2B7 was the main enzyme involved in its glucuronidation
All values represent the geometric mean of three independent experiments (unless otherwise indicated).
| Compound | Relative Vmax | Km | Ki |
|---|---|---|---|
| peak area of glucuronide/mg protein/min | μM | ||
| Alprazolam | 169 | 261 | N.A. |
| Fluconazole | 158 | 1667 | N.A. |
| Itraconazole | No data | No data | No data |
| Voriconazole | 436 | 1130 | N.A. |
| Tioconazole | 31445 | 124 | 245 |
| Ketoconazole | 541 (n = 2) | 7 (n = 2) | 941 (n = 2) |
| Econazole | 6532 | 115 | 192 |
| Miconazole | 7513 | 58.7 | 475 |
| Bifonazole | 13268 | 28 | 47 |
| Sulconazole | 4902 | 35 | 290 |
N.A., not applicable.