Interaction of the Efflux Transporters ABCB1 and ABCG2 With Imatinib, Nilotinib, and Dasatinib

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, othe...

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Bibliographic Details
Published in:Clinical pharmacology and therapeutics 2014-03, Vol.95 (3), p.294-306
Main Authors: Eadie, L N, Hughes, T P, White, D L
Format: Article
Language:English
Subjects:
Animals
ATP Binding Cassette Transporter, Subfamily B
ATP Binding Cassette Transporter, Subfamily B, Member 1 - metabolism
ATP Binding Cassette Transporter, Subfamily G, Member 2
ATP-Binding Cassette Transporters - metabolism
Benzamides - metabolism
Biological and medical sciences
Dasatinib
Enzyme Inhibitors - metabolism
Humans
Imatinib Mesylate
Medical sciences
Neoplasm Proteins - metabolism
Pharmacology. Drug treatments
Piperazines - metabolism
Protein-Tyrosine Kinases - antagonists & inhibitors
Pyrimidines - metabolism
Thiazoles - metabolism
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Summary: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. Clinical Pharmacology & Therapeutics (2014); 95 3, 294–306. doi:10.1038/clpt.2013.208
ISSN:0009-9236
1532-6535
DOI:10.1038/clpt.2013.208