Title:Development of the Third Generation EGFR Tyrosine Kinase Inhibitors for Anticancer Therapy
Volume: 23
Issue: 29
Author(s): Weiyan Cheng, Jianhua Zhou, Xin Tian, Xiaojian Zhang
Affiliation:
关键词:
Anticancer
摘要: 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.
