EAI045: the Fourth-generation EGFR Inhibitor Overcoming T790M and C797S Resistance
The third-generation tyrosine kinase inhibitors (TKI), AZD9291 (osimertinib) and CO-1686 (rociletinib) of epidermal growth factor receptor (EGFR) are highly active against T790M positive non-small cell lung cancer (NSCLC). However, resistance develops rapidly. EGFR C797S mutation was reported to be a leading mechanism of resistance to the third-generation inhibitors. The C797S mutation appears to be an ideal target for overcoming the acquired resistance to the third-generation inhibitors. This review summarizes the latest development on the discovery of a fourth-generation EGFR TKI, EAI045.3.
Wang, S., Song, Y., & Liu, D. (2017). EAI045: the Fourth-generation EGFR Inhibitor Overcoming T790M and C797S Resistance. Cancer Letters, 385, 51-54. https://doi.org/10.1016/j.canlet.2016.11.008