TABLE 3

CLint of prednisolone, warfarin, and theophylline in HepaRG cells

Major metabolic routes and CLint (µl/min/106 cells) ± S.D. of prednisolone, warfarin, and theophylline in HepaRG and HepaRG-CAR cells cultured without or with DMSO. No reliable clearance of theophylline could be detected. Prednisolone, warfarin, and theophylline were determined respectively in three, four, and one independent experiment with three separate samples each.

DrugMetabolismHepaRG (DMSO−)HepaRG-CAR (DMSO-)HepaRG (DMSO+)HepaRG-CAR (DMSO+)
PrednisoloneCYP3A40.12 ± 0.080.12 ± 0.060.20 ± 0.130.33 ± 0.11*, ***,****
WarfarinCYP2C9 > CYP3A40.32 ± 0.170.39 ± 0.140.28 ± 0.080.59 ± 0.14 *, **,*****
TheophyllineCYP1A2NDNDNDND

  • ND, not determined.

  • ↵* P < 0.001 versus HepaRG (DMSO-); **P < 0.01; ***P < 0.001 versus HepaRG-CAR (DMSO-); ****P < 0.05; *****P < 0.001 versus HepaRG (DMSO+).