Reversible inhibition kinetics of BG and DHB toward CYP3A4 catalytic activity in HIM and cDNA-expressed CYP3A4.
CYP3A Substrate | Enzyme Source | S50a or Kmb | Vmax | CLint | Ki | ||
|---|---|---|---|---|---|---|---|
| BG | DHB | ||||||
| μM | μM | ||||||
| Testosterone | HIM | 48 | 1.7 nmol/min/mg | 35 μl/min/mg | 1.6 | 0.7 | |
| CYP3A4 | 22 | 99 pmol/min/pmol | 4.6 μl/min/pmol | 0.5 | 0.4 | ||
| Midazolam | HIM | 2.1 | 0.72 nmol/min/mg | 350 μl/min/mg | 13.3 | 0.9 | |
|
| CYP3A4 | 1.8 | 49 pmol/min/pmol | 28 μl/min/pmol | 6.1 | 0.5 | |