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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Review Article

Development of the Third Generation EGFR Tyrosine Kinase Inhibitors for Anticancer Therapy

Author(s): Weiyan Cheng, Jianhua Zhou, Xin Tian and Xiaojian Zhang

Volume 23, Issue 29, 2016

Page: [3343 - 3359] Pages: 17

DOI: 10.2174/0929867323666160510123604

Price: $65


Epidermal growth factor receptor (EGFR) is one of the most important targets in anticancer therapy. Till date, a large number of first and second generation EGFR tyrosine kinase inhibitors (TKIs) have been marketed or advanced into clinical studies. However, the occurrence of TKI-resistant mutations has led to the loss of efficacy of these inhibitors. In the purpose of overcoming resistant mutations and reducing side effects, lots of third generation EGFR inhibitors are explored with promising potencies against EGFR mutations while sparing wild-type EGFR. This review outlines the current landscape of the development of third generation EGFR inhibitors, mainly focusing on the biological properties, clinical status and structure-activity relationships.

Keywords: Anticancer, Clinical, EGFR, Mutation, Small molecule inhibitor, Third generation.

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