Kinetic parameters for cDNA-expressed CYP3A4 (Supersomes)-mediated metabolism of ITZ, OH-ITZ, and keto-ITZ
Km ± S.D. | fu ± S.D. | Km,u | kdep[S]→0 ± S.D. | Vmax | CLint,u | |
|---|---|---|---|---|---|---|
| nM | % | nM | 1/min | pmol/min/nmol 3A4 | ml/min/nmol CYP3A4 | |
| ITZ | 44.4 ± 11.1 | 8.8 ± 3.2 | 3.9 | 0.69 ± 0.07 | 270 | 69.3 |
| OH-ITZ | 71.7 ± 37.5 | 38 ± 20 | 27 | 0.33 ± 0.06 | 543 | 19.8 |
| keto-ITZ | 17.9 ± 8.8 | 9.2 ± 4.9 | 1.4 | 0.63 ± 0.18 | 86.9 | 62.5 |