Osimertinib (AZD9291) Attenuates the Function of Multidrug Resistance-Linked ATP-Binding Cassette Transporter ABCB1 in Vitro

作者: Sung-Han Hsiao , Yu-Jen Lu , Yan-Qing Li , Yang-Hui Huang , Chia-Hung Hsieh

DOI: 10.1021/ACS.MOLPHARMACEUT.6B00249

关键词:

摘要: The effectiveness of cancer chemotherapy is often circumvented by multidrug resistance (MDR) caused the overexpression ATP-binding cassette (ABC) drug transporter ABCB1 (MDR1, P-glycoprotein). Several epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) have been shown previously capable modulating function and reversing ABCB1-mediated MDR in human cells. Furthermore, some TKIs are transported ABCB1, which results low oral bioavailability, reduced distribution, development acquired to these TKIs. In this study, we investigated interaction between osimertinib, a novel selective, irreversible third-generation EGFR TKI that has recently approved U.S. Food Drug Administration. We also evaluated potential impact on efficacy osimertinib cells, can present therapeutic challenge clinicians future. revealed although stimulates ATPase act...

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