Journal of Hematology & Oncology (Jul 2016)

EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer

  • Shuhang Wang,
  • Stella T. Tsui,
  • Christina Liu,
  • Yongping Song,
  • Delong Liu

DOI
https://doi.org/10.1186/s13045-016-0290-1
Journal volume & issue
Vol. 9, no. 1
pp. 1 – 5

Abstract

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Abstract 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.