TABLE 2

Correlation of DY-9760e metabolism with specific P450 isozyme activity in human liver microsomes from 16 individual donors

P450 Isozyme Activity
P450
Correlation Coefficient (r)
M3
M5
M6
M7
M8
DY-9836
7-Ethoxyresorfin O-dealkylation CYP1A2 0.003 -0.230 -0.067 0.078 0.009 0.020
Coumarin 7-hydroxylation CYP2A6 0.218 0.465 0.206 0.124 0.194 0.137
(S)-Mephenytoin N-demethylation CYP2B6 0.539* 0.472 0.412 0.443 0.438 0.420
Paclitaxel 6α-hydroxylation CYP2C8 0.682** 0.364 0.377 0.522* 0.550* 0.503*
Diclofenac 4′-hydroxylation CYP2C9 0.358 0.860*** 0.219 0.245 0.309 0.231
(S)-Mephenytoin 4′-hydroxylation CYP2C19 0.357 0.161 0.372 0.369 0.365 0.362
Dextromethorphan O-demethylation CYP2D6 0.184 0.124 0.050 0.115 0.117 0.087
Chlorzoxazone 6-hydroxylation CYP2E1 -0.015 0.211 -0.235 -0.181 -0.115 -0.161
Testosterone 6β-hydroxylation CYP3A4/5 0.958*** 0.215 0.947*** 0.973*** 0.957*** 0.966***
Lauric acid 12-hydroxylation
CYP4A9/11
0.160
0.188
0.031
0.210
0.138
0.132

  • ↵* p < 0.05; ** p < 0.01; *** p < 0.001.