TABLE 4

Inactivation kinetics of BG and DHB toward CYP3A4 catalytic activity in human in HIM and cDNA-expressed CYP3A4


CYP3A Substrate

Enzyme Source

KI

kinact

kinact/KI
BG
DHB
BG
DHB
BG
DHB
μM min−1 μl/min/pmol
Testosterone HIM 28.6 2.5 0.34 0.40 12 160
CYP3A4 3.1 1.7 0.47 0.52 150 305
Midazolam HIM 23.5 3.5 0.36 0.31 15 89

CYP3A4
1.9
1.1
0.70
0.41
370
373