Sirolimus oral absorption in rats is increased by ketoconazole but is not affected by D-alpha-tocopheryl poly(ethylene glycol 1000) succinate.

@article{Wacher2002SirolimusOA,
  title={Sirolimus oral absorption in rats is increased by ketoconazole but is not affected by D-alpha-tocopheryl poly(ethylene glycol 1000) succinate.},
  author={Vincent J. Wacher and Jeffrey A. Silverman and Susan Wong and Paulina Tran-Tau and Amy O Chan and Anne Chai and Xiang-qing Yu and Daniel P. O'Mahony and Zeibun Ramtoola},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2002},
  volume={303 1},
  pages={308-13}
}
The contributions of cytochrome P450 3A (CYP3A) and P-glycoprotein to sirolimus oral bioavailability in rats were evaluated by coadministration of sirolimus (Rapamune) with the CYP3A inhibitor ketoconazole or the P-glycoprotein inhibitor D-alpha-tocopheryl poly(ethylene glycol 1000) succinate (TPGS). Groups of six male Sprague-Dawley rats (250-300 g) were administered Rapamune (1 mg/kg) by oral gavage, alone and with ketoconazole (30 mg/kg) or TPGS (50 mg/kg). Sirolimus levels were measured in… CONTINUE READING