Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941.

@article{Salphati2010RoleOP,
  title={Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941.},
  author={Laurent Salphati and Leslie B. Lee and Jodie Pang and Emile G Plise and Xiaolin Zhang},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2010},
  volume={38 9},
  pages={1422-6}
}
2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) is a novel small molecule inhibitor of the phosphatidylinositol 3-kinase (PI3K) pathway currently evaluated in the clinic as an anticancer agent. The objectives of this study were to determine in vitro whether GDC-0941 was a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (Bcrp1) and to investigate the impact of these transporters on the pharmacokinetics… CONTINUE READING
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PGlycoprotein and breast cancer resistance protein: two dominant transporters working together in limiting the brain penetration of topotecan

  • NA de Vries, J Zhao, E Kroon, T Buckle, JH Beijnen, O van Tellingen
  • Clin Cancer Res
  • 2007
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