The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients.

@article{Breedveld2005TheEO,
  title={The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients.},
  author={Pauline Breedveld and Dick Pluim and Greta Cipriani and Peter R. Wielinga and Olaf van Tellingen and Alfred H. Schinkel and Jan H. M. Schellens},
  journal={Cancer research},
  year={2005},
  volume={65 7},
  pages={
          2577-82
        }
}
Imatinib mesylate (signal transduction inhibitor 571, Gleevec) is a potent and selective tyrosine kinase inhibitor, which was shown to effectively inhibit platelet-derived growth factor-induced glioblastoma cell growth preclinically. However, in patients, a limited penetration of imatinib into the brain has been reported. Imatinib is transported in vitro and in vivo by P-glycoprotein (P-gp; ABCB1), which thereby limits its distribution into the brain in mice. Previously, imatinib was shown to… Expand
Influence of breast cancer resistance protein (Abcg2) and p‐glycoprotein (Abcb1a) on the transport of imatinib mesylate (Gleevec®) across the mouse blood–brain barrier
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