The effects of gefitinib on the apparent kinetic parameters for NPC and APC formation by CYP3A4 in human small intestinal microsomes
Gefitinib | NPC Formation | APC Formation | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Km | Vmax | CLint | Km | Vmax | CLint | |||||
| μM | pmol/min/mg protein | μl/min/mg protein | μM | pmol/min/mg protein | μl/min/mg protein | |||||
| 0 μM | 49 | 15 | 0.31 | 59 | 6.7 | 0.11 | ||||
| 5 μM | 52 | 11 | 0.21 | 114 | 9.9 | 0.087 | ||||
| 10 μM | 64 | 12 | 0.19 | 97 | 12 | 0.12 | ||||
| 20 μM | 67 | 11 | 0.16 | 73 | 15 | 0.21 | ||||
| 40 μM | 106 | 15 | 0.14 | 91 | 28 | 0.31 | ||||