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Expert Opin Investig Drugs. 2014 Oct;23(10):1333-48. doi: 10.1517/13543784.2014.928283. Epub 2014 Jun 12.

Small-molecule EGFR tyrosine kinase inhibitors for the treatment of cancer.

Author information

1
Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes , 35 Keyan Rd., Zhunan, Miaoli County 350, ROC , Taiwan +886 37 246 166 Ext. 35708 ; +886 37 586 456 ; hphsieh@nhri.org.tw.

Abstract

INTRODUCTION:

EGFR has been implicated in various malignancies such as NSCLC, breast, head and neck, and pancreatic cancer. Numerous drugs have been developed in order to target the tyrosine domain of EGFR as an approach in cancer treatment.

AREAS COVERED:

This article focuses on the different generations of EGFR tyrosine kinase inhibitors (TKIs). This spans from the emergence of the first-generation EGFR-TKIs to overcoming drug resistance using second-generation EGFR-TKIs and to reducing adverse effect (AE) using mutant-selective third-generation EGFR-TKIs.

EXPERT OPINION:

Current TKI treatment is frequently accompanied by drug resistance and/or serious AEs. There has been the promise of advancements in second-generation EGFR-TKIs that could overcome drug resistance, acting as second- or third-line salvage treatment, but this promise has yet to be met. That being said, both issues are currently being addressed with mutant-selective EGFR-TKIs with the expectation of bringing more EGFR-targeted therapy into the next phase of cancer therapy in the future.

KEYWORDS:

AZD-9291; CO-1686; EGFR; NSCLC; afatinib; dacomitinib; erlotinib; gefitinib; icotinib

PMID:
24921970
DOI:
10.1517/13543784.2014.928283
[Indexed for MEDLINE]

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