CYP1A2 | CYP2C9 | CYP2C19 | CYP2D6 | CYP3A4 | |
---|---|---|---|---|---|
Correlation Coefficient (r2) | |||||
[S] = 0.3 μM | |||||
Ezlopitant consumption | 0.329 | 0.020 | 0.200 | 0.243 | 0.389 |
CJ-12,458 formation | 0.295 | 0.000 | 0.040 | 0.315 | 0.5982-b |
CJ-12,764 formation | 0.453 | 0.002 | 0.065 | 0.372 | 0.434 |
[S] = 10 μM | |||||
Ezlopitant consumption | 0.347 | 0.005 | 0.044 | 0.280 | 0.6372-b |
CJ-12,458 formation | 0.346 | 0.002 | 0.048 | 0.249 | 0.6272-b |
CJ-12,764 formation | 0.442 | 0.002 | 0.069 | 0.217 | 0.485 |
[S] = 100 μM | |||||
Ezlopitant consumption | 0.256 | 0.001 | 0.137 | 0.063 | 0.466 |
CJ-12,458 formation | 0.326 | 0.004 | 0.016 | 0.174 | 0.7522-b |
CJ-12,764 formation | 0.359 | 0.003 | 0.040 | 0.114 | 0.6572-b |
↵2-a Cytochrome P450 marker activities are as follows:
CYP1A2: phenacetin O-deethylase at [phenacetin] = 50 μM
CYP2C9: tolbutamide hydroxylase at [tolbutamide] = 200 μM
CYP2C19: S-mephenytoin 4′-hydroxylase at [S-mephenytoin] = 200 μM
CYP2D6: bufuralol 1′-hydroxylase at [bufuralol] = 10 μM
CYP3A4: testosterone 6β-hydroxylase at [testosterone] = 50 μM
↵2-b Correlation was statistically significant (P < 0.0005; Student's ttest).