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Updated: May 4, 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
Novel agents and strategies for overcoming EGFR TKIs resistance
1Guangdong Lung Cancer Institute, Guangdong General Hospital & Guangdong Academy of Medical Sciences, Guangzhou, PR China. syylwu@live.cn.
Abstract:
Since the recognition of epidermal growth factor receptor (EGFR) as a therapeutic target, EGFR tyrosine kinase inhibitors (TKIs) have been used in lung cancer patients with EGFR mutations, which has been a major breakthrough for lung cancer treatment.. The progression-free survival (PFS) of patients with EGFR mutations treated with EGFR TKIs is significantly prolonged compared with that of patients who underwent standard chemotherapy. However, all patients who initially respond to EGFR TKIs eventually develop acquired resistance (AR). Many small molecule agents and monoclonal antibodies (McAb) targeting signaling pathways are potential therapeutic regimens for overcoming resistance, and various therapeutic strategies are used in clinical practice. Here we review the novel agents and therapeutic strategies for overcoming AR to EGFR TKIs.
Insights
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) improve lung cancer survival but acquired resistance (AR) develops. This review covers novel agents and strategies to overcome AR in EGFR-mutated lung cancer.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Epidermal growth factor receptor (EGFR) is a key therapeutic target in lung cancer.
- EGFR tyrosine kinase inhibitors (TKIs) significantly improve progression-free survival (PFS) in patients with EGFR mutations.
- Acquired resistance (AR) to EGFR TKIs is an inevitable challenge in lung cancer treatment.
Purpose of the Study:
- To review novel agents for overcoming acquired resistance (AR) to EGFR TKIs.
- To discuss emerging therapeutic strategies for patients with EGFR-mutated lung cancer who develop resistance.
- To provide an overview of current clinical practices for managing AR to EGFR TKIs.
Main Methods:
- Literature review of novel agents targeting signaling pathways.
- Analysis of therapeutic strategies for overcoming acquired resistance (AR).
- Synthesis of information on clinical practices for managing AR to EGFR TKIs.
Main Results:
- EGFR TKIs offer significant PFS benefits but acquired resistance (AR) eventually occurs.
- Various small molecule agents and monoclonal antibodies (McAb) show promise in overcoming AR.
- Multiple therapeutic strategies are being investigated and used in clinical practice.
Conclusions:
- Overcoming acquired resistance (AR) to EGFR TKIs is crucial for improving long-term outcomes in lung cancer.
- Novel agents and therapeutic strategies are essential for managing resistance.
- Continued research into overcoming AR is vital for advancing lung cancer treatment.
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