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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 potently inhibit human breast cancer
resistance protein (BCRP; ABCG2).
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