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Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer

Shuhang Wang1, Shundong Cang2, Delong Liu3,4

  • 1The Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Peking University Cancer Hospital, Beijing, China.

Journal of Hematology & Oncology
|April 14, 2016
PubMed

Insights

Third-generation tyrosine kinase inhibitors (TKIs) target the EGFR T790M mutation, overcoming resistance in non-small cell lung cancer (NSCLC). Osimertinib is approved, while other agents are in development for advanced NSCLC treatment.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are standard treatment for non-small cell lung cancer (NSCLC).
  • The EGFR T790M mutation confers resistance to existing EGFR TKIs, necessitating new therapeutic strategies.
  • Third-generation EGFR TKIs are being developed to overcome this resistance mechanism.

Purpose of the Study:

  • To review emerging data on third-generation EGFR TKIs targeting the T790M mutation.
  • To discuss the clinical development and efficacy of these novel agents in advanced NSCLC.

Main Methods:

  • Review of clinical trial data and published literature on third-generation EGFR TKIs.
  • Focus on agents like osimertinib, rociletinib, HM61713, ASP8273, EGF816, and PF-06747775.

Main Results:

  • Osimertinib and rociletinib demonstrated clinical efficacy in Phase I/II trials for patients with acquired resistance to earlier TKIs.
  • Osimertinib (AZD9291, TAGRISSO) received FDA approval for metastatic EGFR T790M mutation-positive NSCLC.
  • Other agents (HM61713, ASP8237, EGF816, PF-06747775) are in earlier stages of clinical development.

Conclusions:

  • Third-generation EGFR TKIs represent a promising therapeutic approach for NSCLC patients with the T790M resistance mutation.
  • Osimertinib's approval marks a significant advancement, with ongoing development of other agents offering future treatment options.

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