TABLE 1.
Inhibition constants for ABT in suspension human hepatocytes (HHEPs) and recombinant UGTs (rUGTs).
| UGT isoform | Substrate | Substrate concentration (μM) | Ki,u (mM) | |
|---|---|---|---|---|
| HHEPs | rUGTs | |||
| 1A1 | β‐Estradiol | 3 | No inhibition | >20 a |
| 1A3 | CDCA | 2 | 6.03 | 1.90 |
| 1A4 | TFP | 1 | 2.52 | 1.54 |
| 1A6 | Serotonin | 1715 | No inhibition | 15.8 |
| 1A9 | Propofol | 10 | 4.58 | 1.79 |
| 2B7 | Zidovudine | 100 | 5.45 | 3.90 |
| 2B15 | Oxazepam | 10 | >20 b | 7.30 |
a
Up to 59% inhibition was observed in at least one of the triplicate incubations at 20 mM.
b
Up to 45% inhibition was observed in at least one of the triplicate incubations at 20 mM.