TABLE 3

IC50 values (micromolar) for BG and DHB toward testosterone 6β-hydroxylation in HIM and cDNA-expressed CYP3A4


Enzyme Source

Inhibitor





Testosterone Concentration




20 μM 50 μM 100 μM 200 μM 400 μM
HIM BG 0.8 0.7 1.0 1.7 1.9
DHB 0.5 0.5 0.6 0.9 0.9
15 μM 30 μM 60 μM 120 μM 240 μM
CYP3A4 BG 0.4 0.4 0.8 1.5 1.6

DHB
0.4
0.3
0.5
0.6
0.8