Summary of enzyme kinetic parameters of ezlopitant metabolism by heterologously expressed CYP2D6 and CYP3A4
| CYP Isoform/Reaction | KMapp | Vmax | CL′intCalculated for Sf9 Cell Microsomes |
|---|---|---|---|
| μM | nmol/min/ nmol CYP | ml/min/ nmol CYP | |
| CYP2D6: | |||
| CJ-12,458 formation | 0.6 | 1.8 | 3.0 |
| CJ-12,764 formation | 0.4 | 1.9 | 4.8 |
| CYP3A4: | |||
| CJ-12,458 formation | 9.1 | 4.4 | 0.48 |
| CJ-12,764 formation | 11 | 5.8 | 0.53 |
| CYP3A5: | |||
| CJ-12,458 formation | 5.6 | 7.3 | 0.77 |
| CJ-12,764 formation | 7.5 | 18 | 2.4 |