Bafetinib

Bafetinib is a substituted benzamide derivative and tyrosine kinase inhibitor structurally related to STI-571 (Imatinib Mesylate). It is a potent Bcr-Abl kinase inhibitor. Also shown to be a potent and selective inhibitor of Lyn tyrosine kinase, an agent of imatinib-resistant leukemia. Bafetinib significantly sensitised ABCB1 and ABCG2 overexpressing MDR cells to their anticancer substrates and increased the intracellular accumulation of anticancer drugs. Eosinophils play a key role in allergic inflammation, bafetinib inhibits oxidative burst and generation of inflammatory mediators and reverses eosinophil survival.

References

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[6] Zhang, Y., Zhang, G., Wang, Y. et al. Bafetinib (INNO-406) reverses multidrug resistance by inhibiting the efflux function of ABCB1 and ABCG2 transporters. Sci Rep 6, 25694 (2016) https://doi.org/10.1038/srep25694.

[7] Milara, J., Martinez-Lopez, M., Sanz, C., Almudever, P., Peiro, T., Serrano, A., Morcillo, EJ., Zaragoza, C. and Cortijo, J. (2013) 'Bafetinib inhibits functional responses of human eosinophils in vitro', European Journal of Pharmacology, 715(1-3), pp. 172-180.