Target P450 | Inhibitor | Reversible ([I]/Ki)a | Irreversible (λ/kdeg) | ||
---|---|---|---|---|---|
Cmax | Cmax*fu | Cmax | Cmax*fu | ||
CYP2C19 (hepatic) | OMP | 0.080 | 0.0042 | 5.2 | 0.29 |
OH-OMP | 0.012 | 0.0022 | N.D. | N.D. | |
DM-OMP | 0.0008 | 0.0008 | 0.12 | 0.12 | |
OMP-S | 0.028 | 0.0007 | 0.92 | 0.022 | |
COMP | N.D. | N.D. | N.D. | N.D. | |
Total | 0.12 | 0.0078 | 6.25 | 0.44 | |
CYP3A4 (hepatic) | OMP | 0.017 | 0.0009 | 1.23 | 0.065 |
OH-OMP | 0.024 | 0.004 | N.D. | N.D. | |
DM-OMP | 0.002 | 0.002 | 0.11 | 0.11 | |
OMP-S | 0.017 | 0.0004 | N.D. | N.D. | |
COMP | 0.005 | 0.0004 | N.D. | N.D. | |
Total | 0.066 | 0.0074 | 1.34 | 0.18 | |
CYP3A4 (intestinal) | OMP | 6.0 | 6.0 | 50 | 50 |
↵a [I]/Ki is extrapolated from the [I]/IC50 ratio.