New Strategies and Novel Combinations in EGFR TKI-Resistant Non-small Cell Lung Cancer
Related Experiment Video
Updated: Aug 25, 2025

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
1Institut Curie, Institut du Thorax Curie Montsouris, 26 rue d'Ulm, 75005, Paris, France. nicolas.girard2@curie.fr.
Opinion Statement:
Osimertinib is the current standard-of-care for the first-line treatment of Epidermal Growth Factor Receptor (EGFR)-mutant non-small cell lung cancer (NSCLC). Progression after osimertinib ineluctably occurs, and standard of care treatment options beyond progression have mainly included next-line platinum doublet chemotherapy. With better understanding of the varied molecular mechanisms of resistance to osimertinib, several opportunities for the use of targeted agents are emerging that include MET amplification, observed in 15% of patients, and resistant EGFR mutations, including C797S in 7% of patients. Evidence for the use of targeted therapies in such situations is mostly based on case reports, but clinical trials are being conducted with MET inhibitors, such as amivantamab, an EGFR-MET bispecific antibody, or next-generation EGFR inhibitors, such as patritumab-deruxtecan, a HER3 antibody drug conjugate. In this review, we outline our proposed approach to current clinical practice for patients with EGFR mutant, osimertinib-resistant NSCLC which includes the following potential strategies: - Continuation of osimertinib beyond progression following local ablative treatment of oligoprogressive disease, - Tissue rebiopsy of progressive site and possibly concurrent liquid biopsy to evaluate for mechanism of resistance utilizing comprehensive genomic profiling, -Discussion at a molecular tumor board for assessment for enrollment in clinical trials/expanded access program if available with innovative drugs or possible off-label use of available targeted agents, based on the results of molecular profiling, -If no mechanism of resistance identified, administration of platinum-based chemotherapy with antiangiogenic agents. The role of immunotherapy will also be addressed given the uncertain benefit.
Insights
Treatment strategies for Epidermal Growth Factor Receptor (EGFR)-mutant non-small cell lung cancer (NSCLC) progressing after osimertinib are evolving. Rebiopsy and molecular profiling guide targeted therapies or chemotherapy for resistant EGFR-mutant NSCLC.
Area of Science:
- Oncology
- Molecular Biology
- Genomics
Background:
- Osimertinib is the standard first-line treatment for Epidermal Growth Factor Receptor (EGFR)-mutant non-small cell lung cancer (NSCLC).
- Disease progression inevitably occurs, with limited standard treatment options beyond platinum-based chemotherapy.
- Emerging resistance mechanisms, including MET amplification and EGFR mutations like C797S, present opportunities for targeted therapies.
Purpose of the Study:
- To outline a clinical practice approach for managing osimertinib-resistant EGFR-mutant NSCLC.
- To review emerging targeted agents and strategies for overcoming resistance.
- To discuss the role of comprehensive genomic profiling and molecular tumor boards.
Main Methods:
- Review of current literature and clinical trial data on osimertinib resistance mechanisms.
- Proposed strategies include continuation of osimertinib for oligoprogression, rebiopsy (tissue and liquid) for resistance profiling.
- Discussion of targeted agents (e.g., MET inhibitors, next-generation EGFR inhibitors) and chemotherapy.
Main Results:
- MET amplification (15%) and EGFR mutations (e.g., C797S, 7%) are key resistance mechanisms.
- Targeted therapies like amivantamab and patritumab-deruxtecan are under investigation.
- A multidisciplinary approach involving molecular tumor boards is recommended for treatment decisions.
Conclusions:
- Personalized treatment strategies based on molecular profiling are crucial for osimertinib-resistant NSCLC.
- Clinical trials and off-label use of targeted agents offer promising alternatives to chemotherapy.
- Further research is needed to clarify the role of immunotherapy in this setting.
More Related Videos
09:38Establishment and Characterization of Three Afatinib-resistant Lung Adenocarcinoma PC-9 Cell Lines Developed with Increasing Doses of Afatinib
Published on: June 26, 2019
08:52Profiling Sensitivity to Targeted Therapies in EGFR-Mutant NSCLC Patient-Derived Organoids
Published on: November 22, 2021
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against...
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
Mitogens and the Cell Cycle
Treatment Resistant Cancers
Tumor Immunotherapy