Table 3.
Enzyme kinetic parameters for the metabolism of DWP16001 to M1 and M2 in human liver microsomes (HLM) and human recombinant CYP3A4 and CYP2C19 supersomes.
| Enzymes | M1 Formation | M2 Formation | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Km (µM) | V max | Cl int | n | Mode | Km (µM) | V max | Cl int | n | Mode | |
| HLM | 150.1 | 980.3 | 6.531 | 0.9176 | Hill | 58.7 | 82.8 | 1.411 | 0.9773 | Hill |
| CYP3A4 | 471.4 | 28.9 | 0.061 | 0.7505 | Hill | 674.5 | 3.8 | 0.006 | 0.696 | Hill |
| CYP2C19 | 156.4 | 3.6 | 0.023 | - | Single enzyme | 35.4 | 0.688 | 0.019 | 1.3 | Hill |
Vmax: HLM, pmol/min/mg protein; CYP3A4 and CYP2C19, pmol/min/pmol CYP; Clint (Vmax/Km): HLM, μL/min/mg protein; CYP3A4 and CYP2C19, μL/min/pmol CYP; n: hill coefficient.