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Type: Journal article
Title: Interaction of the efflux transporters ABCB1 and ABCG2 with imatinib, nilotinib, and dasatinib
Author: Eadie, L.
Hughes, T.
White, D.
Citation: Clinical Pharmacology & Therapeutics, 2014; 95(3):294-306
Publisher: Mosby
Issue Date: 2014
ISSN: 0009-9236
Statement of
L N Eadie, T P Hughes and D L White
Abstract: 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.
Keywords: Animals; Humans; Benzamides; Piperazines; Pyrimidines; Thiazoles; ATP-Binding Cassette Transporters; Neoplasm Proteins; Enzyme Inhibitors; Protein-Tyrosine Kinases; Imatinib Mesylate; Dasatinib; ATP Binding Cassette Transporter, Sub-Family G, Member 2; ATP Binding Cassette Transporter, Sub-Family B; ATP-Binding Cassette, Sub-Family B, Member 1
Rights: © 2014 American Society for Clinical Pharmacology and Therapeutics
RMID: 0020135647
DOI: 10.1038/clpt.2013.208
Appears in Collections:Medicine publications

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