Four generations of EGFR TKIs associated with different pathogenic mutations in non-small cell lung carcinoma

Abstract

Non-small cell lung carcinoma (NSCLC) is a malignant tumour with poor prognosis and high mortality. Platinum-based dual-agent chemotherapy is the main therapeutic regimen for this disease. In recent years, because of the introduction of molecular targeted therapy, various targeted therapeutic agents against epidermal growth factor receptor (EGFR) have been rapidly developed, which has become a research hotspot for NSCLC treatment. Here, we review the latest studies describing the features and types of EGFR pathogenic mutations, currently established EGFR-tyrosine kinase inhibitors from the first to fourth generation, including their action mechanisms, acquired resistance, and clinical applications, and potential challenges and perspectives that current researchers should address.

Keywords:

• Targeted therapy
• epidermal growth factor receptor
• pathogenic mutations
• epidermal growth factor receptor-tyrosine kinase inhibitors
• non-small cell lung carcinoma

Subject Classification Codes:

• translational medicine
• oncology

Disclosure statement

The authors report no declarations of interest.

Author contributions

Li L and Li R designed and wrote the manuscript. Zhou X and Yao H helped with literature collection and validation. All authors reviewed the manuscript.

Additional information

Funding

This work was supported by the National Natural Science Foundation of China [NSFC 81472787, 81773671 and 81828010]; CAMS Innovation Fund for Medical Sciences [CIFMS 2016-I2M-3-013]; and The Drug Innovation Major Project of China [2018ZX09711001-007-002].