Intravenous-to-oral switch in anticancer chemotherapy: a focus on docetaxel and paclitaxel.

@article{Koolen2010IntravenoustooralSI,
  title={Intravenous-to-oral switch in anticancer chemotherapy: a focus on docetaxel and paclitaxel.},
  author={Stijn L. W. Koolen and Jos H. Beijnen and Jan H. M. Schellens},
  journal={Clinical pharmacology and therapeutics},
  year={2010},
  volume={87 1},
  pages={
          126-9
        }
}
Oral administration of the taxanes docetaxel and paclitaxel is hampered by their affinity for drug transporters, especially ABCB1 (P-glycoprotein, Pgp); extensive first-pass metabolism by cytochrome P450 3A (CYP3A); and poor drug solubility. Preclinical studies in Pgp-deficient and wild-type mice demonstrated that modulation of either Pgp or CYP3A resulted in high systemic exposure to docetaxel or paclitaxel. This concept could successfully be translated to clinical trials. 
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