Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918.

@article{Kruijtzer2002IncreasedOB,
  title={Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918.},
  author={C Marielle F Kruijtzer and Jos H. Beijnen and Hilde Rosing and Wim W ten Bokkel Huinink and Margaret E. Schot and Roxanne C. Jewell and Elaine M Paul and Jan H. M. Schellens},
  journal={Journal of clinical oncology : official journal of the American Society of Clinical Oncology},
  year={2002},
  volume={20 13},
  pages={2943-50}
}
PURPOSE We discovered that breast cancer resistance protein (BCRP), a recently identified adenosine triphosphate-binding cassette drug transporter, substantially limits the oral bioavailability of topotecan in mdr1a/1b(-/-) P-glycoprotein (P-gp) knockout and wild-type mice. GF120918 is a potent inhibitor of BCRP and P-gp. The aim was to increase the bioavailability of topotecan by GF120918. PATIENTS AND METHODS In cohort A, eight patients received 1.0 mg/m(2) oral topotecan with or without… CONTINUE READING
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