中国临床药理学与治疗学2026，Vol.31Issue(3)：420-427,8.DOI:10.12092/j.issn.1009-2501.2026.03.014
治疗METex14跳跃突变非小细胞肺癌新药——谷美替尼
A novel drug for the treatment of METex14 skipping mutation non-small cell lung cancer—Glumetinib
摘要
Abstract
The MET exon 14(METex14)skipping mutation is an important therapeutic target in non-small cell lung cancer(NSCLC).Glumetinib,a highly selective oral MET inhibitor developed in China,has gained approval in China and Japan for treating lo-cally advanced or metastatic NSCLC harboring the METex14 skipping mutation.Preclinically,glume-tinib selectively inhibits c-Met kinase activity and its downstream signaling pathways,demonstrating an inhibition rate exceeding 87.7%against MET-driven tumors.In a pivotal phase II study involving 79 pa-tients with METex14-positive NSCLC,glumetinib treatment yielded an objective response rate(ORR)of 66%and a median progression-free survival(PFS)of 8.5 months.The incidence of grade≥3 treat-ment-related adverse events(TRAEs)was 54%,pri-marily edema,hypoalbuminemia,and transami-nase elevations.Treatment discontinuation due to adverse events occurred in only 8%of patients,in-dicating a manageable safety profile.Glumetinib thus represents a novel and effective therapeutic option for NSCLC patients with METex14 skipping mutations,particularly in managing brain metas-tases.Its clinical application is expanding to include overcoming drug resistance and exploring combina-tion therapies.This paper aims to concisely review Glumetinib's structural properties,pharmacokinet-ics,efficacy,safety profile,drug interactions,and potential in combination therapy.Furthermore,it seeks to outline future applications of this drug,providing a valuable reference for clinical medica-tion selection in NSCLC management.关键词
谷美替尼/非小细胞肺癌/MET外显子14跳跃突变/c-Met抑制剂Key words
glumetinib/non-small cell lung can-cer/MET exon 14 skipping mutation/c-Met inhibitor分类
医药卫生引用本文复制引用
尹晓玉,路明,于泽芳,庞国勋..治疗METex14跳跃突变非小细胞肺癌新药——谷美替尼[J].中国临床药理学与治疗学,2026,31(3):420-427,8.基金项目
河北省2026年度医学科学研究课题计划项目(20260001) （20260001）
