© 2016 The Author(s).T790M mutation is the most common mechanism for resistance to first- and second-generation tyrosine kinase inhibitors (TKI) for epidermal growth factor receptor (EGFR). Several third-generation EGFR mutant selective TKIs are being explored to conquer this resistance. AZD9291 (osimertinib, tagrisso) has been approved for treatment of the metastatic EGFR T790M mutation-positive non-small cell lung cancer. Resistance to AZD9291 has been described. C797S mutation was reported to be a major mechanism for resistance to T790M-targeting EGFR inhibitors. This review summarizes the latest development in identifying the C797S mutation and EAI045, the novel selective inhibitor overcoming the C797S mutant.
Wang, S., Tsui, S. T., Liu, C., Song, Y., & Liu, D. (2016, July 22). EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer. Journal of Hematology and Oncology. BioMed Central Ltd. https://doi.org/10.1186/s13045-016-0290-1