EGFR mutation mediates resistance to EGFR tyrosine kinase inhibitors in NSCLC: From molecular mechanisms to clinical research

被引：136

作者：

Dong, Rui-Fang ^{[1
,2
]}

Zhu, Miao-Lin ^{[3
]}

Liu, Ming-Ming ^{[1
,2
]}

Xu, Yi-Ting ^{[1
,2
]}

Yuan, Liu-Liu ^{[1
,2
]}

Bian, Jing ^{[1
,2
]}

Xia, Yuan-Zheng ^{[1
,2
,4
]}

Kong, Ling-Yi ^{[1
,2
]}

机构：

[1] China Pharmaceut Univ, Sch Tradit Chinese Pharm, Jiangsu Key Lab Bioact Nat Prod Res, 24 Tong Jia Xiang, Nanjing 210009, Peoples R China

[2] China Pharmaceut Univ, Sch Tradit Chinese Pharm, State Key Lab Nat Med, 24 Tong Jia Xiang, Nanjing 210009, Peoples R China

[3] Jiangsu Canc Hosp, Dept Pathol, Nanjing 210009, Peoples R China

[4] Guangxi Med Univ, Minist Educ, Key Lab High Incidence Tumour Prevent & Treatment, Nanning 530021, Peoples R China

来源：

PHARMACOLOGICAL RESEARCH | 2021年 / 167卷

基金：

中国国家自然科学基金;

关键词：

EGFR mutations; NSCLC; EGFR-TKI resistance; Overcoming drug resistance; Future development; CELL LUNG-CANCER; GROWTH-FACTOR RECEPTOR; AFATINIB PLUS CETUXIMAB; EXON; 20; INSERTIONS; ACQUIRED-RESISTANCE; T790M MUTATION; BISPECIFIC ANTIBODY; TUMOR-CELLS; ERLOTINIB RESISTANCE; PROTEIN-DEGRADATION;

D O I：

10.1016/j.phrs.2021.105583

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

With the development of precision medicine, molecular targeted therapy has been widely used in the field of cancer, especially in non-small-cell lung cancer (NSCLC). Epidermal growth factor receptor (EGFR) is a well-recognized and effective target for NSCLC therapies, targeted EGFR therapy with EGFR-tyrosine kinase inhibitors (EGFR-TKIs) has achieved ideal clinical efficacy in recent years. Unfortunately, resistance to EGFR-TKIs inevitably occurs due to various mechanisms after a period of therapy. EGFR mutations, such as T790M and C797S, are the most common mechanism of EGFR-TKI resistance. Here, we discuss the mechanisms of EGFR-TKIs resistance induced by secondary EGFR mutations, highlight the development of targeted drugs to overcome EGFR mutation-mediated resistance, and predict the promising directions for development of novel candidates.

引用

页数：18

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