The Next Wave of EGFR Tyrosine Kinase Inhibitors Enter the Clinic

Katerina Politi; Deborah Ayeni; Thomas Lynch

doi:10.1016/j.ccell.2015.05.012

The Next Wave of EGFR Tyrosine Kinase Inhibitors Enter the Clinic

Cancer Cell. 2015 Jun 8;27(6):751-3. doi: 10.1016/j.ccell.2015.05.012.

Authors

Katerina Politi¹, Deborah Ayeni², Thomas Lynch³

Affiliations

¹ Department of Pathology, Yale University School of Medicine, New Haven, CT 06510, USA; Section of Medical Oncology, Department of Medicine, Yale University School of Medicine, New Haven, CT 06510, USA; Yale Comprehensive Cancer Center, Yale University School of Medicine, New Haven, CT 06510, USA. Electronic address: katerina.politi@yale.edu.
² Department of Pathology, Yale University School of Medicine, New Haven, CT 06510, USA.
³ Section of Medical Oncology, Department of Medicine, Yale University School of Medicine, New Haven, CT 06510, USA; Yale Comprehensive Cancer Center, Yale University School of Medicine, New Haven, CT 06510, USA. Electronic address: thomas.lynch@yale.edu.

PMID: 26058074
DOI: 10.1016/j.ccell.2015.05.012

Abstract

The T790M mutation in EGFR accounts for approximately half of all lung cancer cases with acquired resistance to the current clinical EGFR tyrosine kinase inhibitors. In tyrosine kinase inhibitor-resistant lung tumors, rociletinib and AZD9291 are highly active when T790M is present and modestly active when T790M is absent.

MeSH terms

Carcinoma, Non-Small-Cell Lung / drug therapy*
Carcinoma, Non-Small-Cell Lung / enzymology
Carcinoma, Non-Small-Cell Lung / genetics
Carcinoma, Non-Small-Cell Lung / pathology
ErbB Receptors / antagonists & inhibitors*
ErbB Receptors / genetics
ErbB Receptors / metabolism
Humans
Lung Neoplasms / drug therapy*
Lung Neoplasms / enzymology
Lung Neoplasms / genetics
Lung Neoplasms / pathology
Mutation
Protein Kinase Inhibitors / pharmacology*

Substances

Protein Kinase Inhibitors
EGFR protein, human
ErbB Receptors