Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.

Abstract

The tyrosine kinase inhibitors (TKI) against epidermal growth factor receptor (EGFR) are widely used in patients with non-small cell lung cancer (NSCLC). However, EGFR T790M mutation leads to resistance to most clinically available EGFR TKIs. Third-generation EGFR TKIs against the T790M mutation have been in active clinical development. These agents include osimertinib, rociletinib, HM61713, ASP8273, EGF816, and PF-06747775. Osimertinib and rociletinib have shown clinical efficacy in phase I/II trials in patients who had acquired resistance to first- or second-generation TKIs. Osimertinib (AZD9291, TAGRISSO) was recently approved by FDA for metastatic EGFR T790M mutation-positive NSCLC. HM61713, ASP8237, EGF816, and PF-06747775 are still in early clinical development. This article reviews the emerging data regarding third-generation agents against EGFR T790M mutation in the treatment of patients with advanced NSCLC.

• Authors: Shuhang Wang, Shundong Cang, Delong Liu
• Journal: Journal of hematology & oncology (J Hematol Oncol) Vol. 9 Pg. 34 (Apr 12 2016) ISSN: 1756-8722 [Electronic] England
• PMID: 27071706 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• Acrylamides
• Aniline Compounds
• Piperazines
• Protein Kinase Inhibitors
• Pyrimidines
• osimertinib
• rociletinib
• ErbB Receptors

Topics

• Acrylamides (therapeutic use)
• Aniline Compounds
• Carcinoma, Non-Small-Cell Lung (drug therapy, genetics, pathology)
• Clinical Trials as Topic
• Drug Resistance, Neoplasm (drug effects, genetics)
• ErbB Receptors (antagonists & inhibitors, genetics)
• Humans
• Lung Neoplasms (drug therapy, genetics, pathology)
• Mutation, Missense
• Piperazines (therapeutic use)
• Protein Kinase Inhibitors (therapeutic use)
• Pyrimidines (therapeutic use)