Table 2.
Parameters of enzymatic kinetic parameters of aripiprazole in different CYP2D6 genotypes.
| Parameter | NM | IM | PM | UM | Source |
|---|---|---|---|---|---|
| Km,CYP2D6 (µM) | 26.20 | 26.20 | 26.20 | 26.20 | FDA |
| Kcat,CYP2D6,dehydrogenation (1/min) | 14.99 | 10.49 | 0.00 | 14.99 | Calculated |
| Kcat,CYP2D6,hydroxylation (1/min) | 57.17 | 40.02 | 0.00 | 57. 17 | Calculated |
| Km,CYP3A4 (µM) | 298.00 | 298.00 | 298.00 | 298.00 | FDA |
| Kcat,CYP3A4,dehydrogenation (1/min) | 54.85 | 54.85 | 73.79a | 54.85 | Calculated/parameter identification |
| Kcat,CYP3A4,other (1/min) | 44.24 | 44.24 | 59.38a | 44.24 | Calculated/parameter identification |
Parameter identification refers to the process in which software calculates and determines the parameters that result in the best fit between the simulated values and the observed values.
IM, intermediate metabolizer; Kcat, number describing maximum reaction rates per recombinant enzyme; Km, Michaelis constant; NM, normal metabolizer; PM, poor metabolizer; UM, ultrarapid metabolizer.