TABLE 2

The effects of gefitinib on the apparent kinetic parameters for NPC and APC formation by CYP3A4 in human liver 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 44 128 2.9 68 46 0.68
5 μM 48 85 1.8 47 45 0.96
10 μM 46 73 1.6 54 61 1.1
20 μM 49 58 1.2 51 64 1.3
40 μM
93
69
0.74
159
153
0.96