PET-CT imaging with [(18)F]-gefitinib to measure Abcb1a/1b (P-gp) and Abcg2 (Bcrp1) mediated drug-drug interactions at the murine blood-brain barrier.

@article{Vlaming2015PETCTIW,
  title={PET-CT imaging with [(18)F]-gefitinib to measure Abcb1a/1b (P-gp) and Abcg2 (Bcrp1) mediated drug-drug interactions at the murine blood-brain barrier.},
  author={Maria L. H. Vlaming and Tilman L{\"a}ppchen and Harm T. Jansen and Suzanne Kivits and A P G Pieter van Driel and Evita van de Steeg and Jos{\'e} W. A. van der Hoorn and Charles F. Sio and Oliver C Steinbach and Jeroen Degroot},
  journal={Nuclear medicine and biology},
  year={2015},
  volume={42 11},
  pages={833-41}
}
INTRODUCTION The efflux transporters P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP, ABCG2) are expressed at the blood-brain barrier (BBB), and can limit the access of a wide range of drugs to the brain. In this study we developed a PET-CT imaging method for non-invasive, quantitative analysis of the effect of ABCB1 and ABCG2 on brain penetration of the anti-cancer drug gefitinib, and demonstrated the applicability of this method for identification and quantification of… CONTINUE READING
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