Downregulation of hepatic CYP3A isoforms by bardoxolone methyl in rats and its impact on in vivo metabolic capacity reflecting pharmacokinetics

/F), a measure of inherent in vivo metabolic capacity, leading to increases in AUC and bioavailability. No significant alterations in liver weight or plasma hepatic markers were observed. In conclusion, we suggest that hepatic CYP3A expression and intrinsic metabolic capacity are suppressed by BX, thereby markedly increasing the oral bioavailability of CYP3A substrates. These findings may help in the early detection of clinically significant drug interactions between Nrf2 activators and CYP3A substrate drugs.