Targeting MET in EGFR-Mutated NSCLC

Stephanie P L Saw1, Molly S C Li2, Sehhoon Park3

  • 1Division of Medical Oncology, National Cancer Centre Singapore, Singapore.

Insights

MET alterations cause resistance to EGFR tyrosine kinase inhibitors (TKIs) in EGFR-mutated non-small cell lung cancer (NSCLC). Targeting both EGFR and MET offers a promising strategy, but challenges in diagnosis and treatment sequencing remain.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • MET alterations (amplification, overexpression) are key resistance mechanisms to EGFR TKIs in EGFR-mutated NSCLC.
  • MET dysregulation activates oncogenic signaling, justifying dual EGFR and MET inhibition.

Purpose of the Study:

  • Review strategies for targeting MET alterations in EGFR-mutated NSCLC.
  • Emphasize clinical relevance of differentiating MET amplification from c-MET overexpression.
  • Discuss diagnostic and therapeutic approaches.

Main Methods:

  • Review of current literature on MET-targeted therapies in EGFR-mutated NSCLC.
  • Analysis of diagnostic strategies: FISH, NGS, IHC, ctDNA assays.
  • Evaluation of clinical data for TKIs, ADCs, and bispecific antibodies.

Main Results:

  • Dual inhibition of EGFR and MET is a rational approach.
  • Various diagnostic methods exist, each with limitations (e.g., ctDNA assays).
  • Clinical data support EGFR- and MET-directed therapies across different classes.

Conclusions:

  • Distinguishing MET amplification from c-MET overexpression is clinically relevant.
  • Unresolved challenges include biomarker standardization, optimal timing, and sequencing of therapies.
  • Improved biomarker precision and optimized strategies are crucial for maximizing treatment benefits.

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