治疗METex14跳跃突变非小细胞肺癌新药——谷美替尼OA
A novel drug for the treatment of METex14 skipping mutation non-small cell lung cancer—Glumetinib
MET 外显子 14(METex14)跳跃突变是非小细胞肺癌(non-small-cell carcinoma,NSCLC)的重要治疗靶点.谷美替尼是一款中国研发的高选择性口服 MET 抑制剂,已相继在中国和日本获批用于 METex14跳跃突变局部晚期或转移性NSCLC 治疗.谷美替尼能够特异性抑制 c-Met 激酶活性及下游信号通路,临床前研究显示其对MET 驱动型肿瘤抑制率超 87.7%.关键Ⅱ期研究中的 79例 METex14阳性 NSCLC 患者经谷美替尼治疗后的总体客观缓解率达 66%,中位无进展生存期达 8.5个月.≥3级治疗相关不良事件发生率 54%,主要包含水肿、低白蛋白血症及转氨酶升高,仅 8%的患者因不良事件停药,安全性可控.谷美替尼为 METex14跳跃突变 NSCLC 提供了新的高效的治疗选择,特别是对脑转移控制方面优势显著,其临床应用正拓展至耐药逆转及联合治疗领域.本文拟对谷美替尼的结构特性、药动学、有效性、安全性、相互作用、联合治疗等方面进行总结,并对该药物的未来应用前景加以展望,以期为临床治疗 NSCLC 的药物选择提供参考.
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.
尹晓玉;路明;于泽芳;庞国勋
河北医科大学药学院,石家庄 050017,河北||河北省人民医院药学部,石家庄 050051,河北||河北省临床药学重点实验室,石家庄 050051,河北河北医科大学第二医院药学部,石家庄 050052,河北河北省人民医院药学部,石家庄 050051,河北||河北省临床药学重点实验室,石家庄 050051,河北河北医科大学药学院,石家庄 050017,河北||河北省人民医院药学部,石家庄 050051,河北||河北省临床药学重点实验室,石家庄 050051,河北
医药卫生
谷美替尼非小细胞肺癌MET外显子14跳跃突变c-Met抑制剂
glumetinibnon-small cell lung can-cerMET exon 14 skipping mutationc-Met inhibitor
《中国临床药理学与治疗学》 2026 (3)
420-427,8
河北省2026年度医学科学研究课题计划项目(20260001)
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