Camptothecin attenuates cytochrome P450 3A4 induction by blocking the activation of human pregnane X receptor.

@article{Chen2010CamptothecinAC,
  title={Camptothecin attenuates cytochrome P450 3A4 induction by blocking the activation of human pregnane X receptor.},
  author={Yakun Chen and Yong Tang and Gregory T. Robbins and Daotai Nie},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2010},
  volume={334 3},
  pages={999-1008}
}
Differential regulation of drug-metabolizing enzymes (DMEs) is a common cause of adverse drug effects in cancer therapy. Due to the extremely important role of cytochrome P450 3A4 (CYP3A4) in drug metabolism and the dominant regulation of human pregnane X receptor (hPXR) on CYP3A4, finding inhibitors for hPXR could provide a unique tool to control drug efficacies in cancer therapy. Camptothecin (CPT) was demonstrated as a novel and potent inhibitor (IC(50) = 0.58 microM) of an hPXR-mediated… CONTINUE READING