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Updated: Apr 6, 2026

Establishing Dual Resistance to EGFR-TKI and MET-TKI in Lung Adenocarcinoma Cells In Vitro with a 2-step Dose-escalation Procedure
Published on: August 11, 2017
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.
Abstract:
MET alterations, mainly gene amplification and protein overexpression, represent a major mechanism of primary and acquired resistance to EGFR tyrosine kinase inhibitors in EGFR-mutated (EGFRm) NSCLC. Both de novo and acquired MET dysregulation can activate downstream oncogenic signaling, providing a strong rationale for dual inhibition of EGFR and MET. This review summarizes the data for targeting MET alterations in EGFRm NSCLC, with emphasis on the clinical relevance of distinguishing MET amplification from c-MET overexpression. We discuss contemporary diagnostic strategies, including tissue-based fluorescence in situ hybridization, next-generation sequencing, and immunohistochemistry, and the limitations of circulating tumor DNA (ctDNA) assays. We then review the clinical data supporting EGFR- and MET-directed approaches across the therapeutic classes, including tyrosine kinase inhibitors, antibody-drug conjugates, and bispecific antibodies. Finally, we highlight unresolved challenges including the lack of standardized biomarker thresholds, optimal timing of MET inhibition, and rational sequencing of available agents. As the therapeutic landscape continues to evolve, improved biomarker precision and optimization of treatment strategies will be essential to maximize the benefit of MET-targeted therapies in EGFRm NSCLC.
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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