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Imatinib mesylate is a selective tyrosine kinase inhibitor that is
successfully used in the treatment of Philadelphia-positive chronic and acute
leukaemia's, and gastrointestinal stromal tumors. We investigated whether the
intended chronic oral administration of imatinib might lead to the induction of
the intestinal ABC transport proteins ABCB1, ABCC1 (MRP1), ABCC2 (MRP2) and
ABCG2. Using Caco2 cells as an in vitro model for intestinal drug transport, we
found that continuous exposure (up to 100 days) with imatinib (10 muM)
specifically upregulates the _expression_ of ABCG2 (maximal approximately 17-fold)
and ABCB1 (maximal approximately 5-fold).
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