TC50 × Cmax values of amiodarone, acetaminophen, indomethacin, and dextromethorphan
Major metabolic routes, human Cmax values and TC50 values of amiodarone, acetaminophen, indomethacin, and dextromethorphan in HepaRG and HepaRG-CAR cells.
| Drug | Metabolism | Cmax (µM) | HepaRG TC50 (×Cmax) | HepaRG-CAR TC50 (×Cmax) |
|---|---|---|---|---|
| Amiodarone | CYP3A4, CYP2C8 | 0.807 | 47.5 | 60.0* |
| Acetaminophen | Glucuronidation, sulfation > CYP2E1, CYP3A4 | 139 | 122 | 216** |
| Indomethacin | CYP2C9 | 5.59 | 191 | 216 |
| Dextromethorphan | CYP2D6 > CYP3A4 | 0.021 | ND | ND |
ND, not determined.
↵* P < 0.05; **P < 0.001 versus HepaRG.