欢迎访问《中国临床药理学与治疗学》杂志官方网站,今天是

中国临床药理学与治疗学 ›› 2026, Vol. 31 ›› Issue (3): 420-427.doi: 10.12092/j.issn.1009-2501.2026.03.014

• 综述与讲座 • 上一篇    下一篇

治疗METex14跳跃突变非小细胞肺癌新药——谷美替尼

尹晓玉1,2,3(), 路明4, 于泽芳2,3, 庞国勋1,2,3,*()   

  1. 1. 河北医科大学药学院,石家庄 050017,河北
    2. 河北省人民医院药学部,石家庄 050051,河北
    3. 河北省临床药学重点实验室,石家庄 050051,河北
    4. 河北医科大学第二医院药学部,石家庄 050052,河北
  • 收稿日期:2025-06-17 修回日期:2025-08-11 出版日期:2026-03-26 发布日期:2026-04-03
  • 通讯作者: 庞国勋 E-mail:xiaoyu020092@163.com;13503291608@163.com
  • 作者简介:尹晓玉,女,硕士研究生,主管药师,研究方向:临床药学。E-mail:xiaoyu020092@163.com
  • 基金资助:
    河北省2026年度医学科学研究课题计划项目(20260001)

A novel drug for the treatment of METex14 skipping mutation non-small cell lung cancer—Glumetinib

Xiaoyu YIN1,2,3(), Ming LU4, Zefang YU2,3, Guoxun PANG1,2,3,*()   

  1. 1. College of Pharmacy, Hebei Medical University, Shijiazhuang 050017, Hebei, China
    2. Department of Pharmacy,Hebei General Hospital, Shijiazhuang 050051, Hebei, China
    3. Hebei Key Laboratory of Clinical Pharmacy, Shijiazhuang 050051, Hebei, China
    4. Department of Pharmacy, The Second Hospital of Hebei Medical University, Shijiazhuang 050052, Hebei, China
  • Received:2025-06-17 Revised:2025-08-11 Online:2026-03-26 Published:2026-04-03
  • Contact: Guoxun PANG E-mail:xiaoyu020092@163.com;13503291608@163.com

摘要:

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。

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

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 locally advanced or metastatic NSCLC harboring the METex14 skipping mutation. Preclinically, glumetinib 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 patients 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 treatment-related adverse events (TRAEs) was 54%, primarily edema, hypoalbuminemia, and transaminase elevations. Treatment discontinuation due to adverse events occurred in only 8% of patients, indicating a manageable safety profile. Glumetinib thus represents a novel and effective therapeutic option for NSCLC patients with METex14 skipping mutations, particularly in managing brain metastases. Its clinical application is expanding to include overcoming drug resistance and exploring combination therapies. This paper aims to concisely review Glumetinib's structural properties, pharmacokinetics, 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 medication selection in NSCLC management.

Key words: glumetinib, non-small cell lung cancer, MET exon 14 skipping mutation, c-Met inhibitor

中图分类号: