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