Interaction of the Efflux transporters ABCB1 and ABCG2 with imatinib, nilotinib, and dasatinib

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The efflux transporters adenosine triphosphate (ATP)-binding cassette (ABC)B1 and ABCG2 have been demonstrated to interact with the tyrosine kinase inhibitors (TKIs) imatinib, nilotinib, and dasatinib. However, although some studies conclude that TKIs are substrates of one or both transporters, other studies demonstrate only an inhibitory function. This variation is probably due to differences in the concentration of TKIs assayed and the experimental systems used. This article examines the evidence for clinically relevant interactions between three currently approved TKIs and ABCB1/ABCG2.

Original languageEnglish
Pages (from-to)294-306
Number of pages13
JournalClinical Pharmacology and Therapeutics
Issue number3
Publication statusPublished or Issued - 1 Mar 2014

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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