Primary and Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-small Cell Lung Cancer: An Update

被引：49

作者：

Ayoola, Ayodele ^{[1
]}

Barochia, Amit ^{[1
]}

Belani, Kiran ^{[2
]}

Belani, Chandra P. ^{[1
]}

机构：

[1] Penn State Milton S Hershey Med Ctr, Penn State Hershey Canc Inst, Hershey, PA 17033 USA

[2] Univ Maryland, Sch Med, Baltimore, MD 21201 USA

来源：

CANCER INVESTIGATION | 2012年 / 30卷 / 05期

关键词：

EGFR; NCSLC; Acquired resistance; Primary resistance; EPITHELIAL-MESENCHYMAL TRANSITIONS; PREVIOUSLY TREATED PATIENTS; RANDOMIZED PHASE-II; PAN-ERBB INHIBITOR; EGF RECEPTOR; GEFITINIB RESISTANCE; C-MET; GENE AMPLIFICATION; T790M MUTATIONS; COPY NUMBER;

D O I：

10.3109/07357907.2012.666691

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

Epidermal growth factor receptor (EGFR) is a critical target in the treatment of nonsmall cell lung cancer (NSCLC). The mutations involving EGFR are more prevalent in patients of Asian ancestry, women, never smokers, and those with adenocarcinoma histology. Primary mechanism of resistance to EGFR-TKIs includes in frame insertion mutation in exon 20, de novo T790M mutation also on exon 20, activating mutations in KRAS, loss of PTEN, and amplification of c-MET whereas acquired resistance results from development of secondary alteration in ATP domain of T790M. There are many novel targeting agents in development to overcome resistance to EGFR TKIs.

引用

页码：433 / 446

页数：14

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