摘要
表皮生长因子受体(EGFR)是抗肿瘤治疗中最重要的靶点之一。到目前为止,大量的第一代和第二代针对表皮生长因子受体的酪氨酸激酶抑制剂(TKIs)已上市或进入临床研究阶段。然而,TKI耐药突变的发生导致了这些抑制剂的药效的降低。为了克服耐药突变和减少副作用,许多第三代EGFR抑制剂都从具有良好的抗EGFR突变的效力方面去研发而不同于野生型的EGFR。本文概述了第三代EGFR抑制剂的发展现状,主要关注了生物学特性、临床状态和构效关系。
关键词: Anticancer
Current Medicinal Chemistry
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.
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Cite this article as:
Weiyan Cheng, Jianhua Zhou, Xin Tian, Xiaojian Zhang , Development of the Third Generation EGFR Tyrosine Kinase Inhibitors for Anticancer Therapy, Current Medicinal Chemistry 2016; 23 (29) . https://dx.doi.org/10.2174/0929867323666160510123604
DOI https://dx.doi.org/10.2174/0929867323666160510123604 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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