EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance

  • Cancer Lett. 2017 Jan 28;385:51-54. doi: 10.1016/j.canlet.2016.11.008.
Shuhang Wang  1 ,  Yongping Song  2 ,  Delong Liu  3
Affiliations
  • 1. The Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Peking University Cancer Hospital, Beijing, China.
  • 2. Henan Cancer Hospital and the Affiliated Cancer Hospital of Zhengzhou University, 127 Dongming Road, Zhengzhou 450008, China.
  • 3. Henan Cancer Hospital and the Affiliated Cancer Hospital of Zhengzhou University, 127 Dongming Road, Zhengzhou 450008, China. Electronic address: [email protected].
PMID: 27840244 DOI: 10.1016/j.canlet.2016.11.008
Abstract

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.

Keywords
AZD9291; EAI045; EGFR; NSCLC; Rociletinib; TKI; epidermal growth factor receptor; non-small cell lung cancer; tyrosine kinase inhibitor.
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