Table 5 Induction of CYP3A4 mRNA expression in human hepatocytes
From: Alflutinib (AST2818), primarily metabolized by CYP3A4, is a potent CYP3A4 inducer
Test compound | Concentration (μM) | Maximum fold induction | EC50 (μM) | R3 | ||||||
|---|---|---|---|---|---|---|---|---|---|---|
DJJ | QBU | HVN | DJJ | QBU | HVN | DJJ | QBU | HVN | ||
Alflutinib | 0.003–5 | 9.24 | 11.2 | 10.4 | 0.25 | 0.24 | 0.25 | 0.31 | 0.26 | 0.28 |
AST5902 | 0.003–5 | 1.79 | 4.71 | 3.42 | 0.29 | 0.13 | 0.68 | 0.78 | 0.42 | 0.80 |
Rifampin | 10 | 7.22 | 19.4 | 9.46 | 0.1–0.33 | 0.12 | 0.05 | 0.10 | ||
