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

J Drug Target. 2020 Nov;28(9):861-872. doi: 10.1080/1061186X.2020.1737934. Epub 2020 Mar 12.

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; epidermal growth factor receptor-tyrosine kinase inhibitors; non-small cell lung carcinoma; oncology; pathogenic mutations; translational medicine.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Clinical Trials as Topic
  • Drug Evaluation, Preclinical
  • Drug Resistance, Neoplasm / genetics
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / genetics
  • Exons
  • Humans
  • Inhibitory Concentration 50
  • Lung Neoplasms / drug therapy*
  • Molecular Targeted Therapy
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use*

Substances

  • Protein Kinase Inhibitors
  • EGFR protein, human
  • ErbB Receptors