Mechanisms of neratinib resistance in HER2-mutant metastatic breast cancer  

作　　者：Lisa D.Eli Shyam M.Kavuri 

机构地区：[1]Translational Medicine and Diagnostics,Puma Biotechnology,Inc.,Los Angeles,CA 90024,USA [2]Lester and Sue Smith Breast Center,Baylor College of Medicine,Houston,TX 77030,USA [3]Department of Medicine,Baylor College of Medicine,Houston,TX 77030,USA

出　　处：《Cancer Drug Resistance》2022年第4期873-881,共9页癌症耐药（英文）

摘　　要：Human epidermal growth factor receptor 2 (HER2) is a major drug target and clinical biomarker in breast cancertreatment. Targeting HER2 gene amplification is one of the greatest successes in oncology, resulting in the use of awide array of HER2-directed agents in the clinic. The discovery of HER2-activating mutations as novel therapeutictargets in breast and other cancers marked a significant advance in the field, which led to the metastatic breast andother solid tumor trials MutHER (NCT01670877), SUMMIT (NCT01953926), and one arm of plasmaMATCH(NCT03182634). These trials reported initial clinical benefit followed by eventual relapse ascribed to eitherprimary or acquired resistance. These resistance mechanisms are mediated by additional secondary genomicalterations within HER2 itself and via hyperactivation of oncogenic signaling within the downstream signaling axis.

关 键 词：Neratinib HER2 ERBB2 estrogen receptor MUTATION 

分 类 号：R73-37[医药卫生—肿瘤]