Drug intelligence / Profile preview

glumetinib

Development stage
Phase 3
Lead developer
Haihe
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Glumetinib is an oral, potent, and highly selective small molecule inhibitor of the receptor-type tyrosine kinase MET (also known as c-MET). It was developed to target tumors with MET alterations such as MET exon 14 skipping mutations and MET gene amplification. Glumetinib demonstrates excellent pharmacokinetic properties including a long half-life and high steady-state trough concentration. Preclinical studies show that it strongly inhibits c-MET kinase activity and induces rapid tumor regression in various lung cancer models with relevant genetic alterations. Clinical trials have shown robust efficacy in non-small cell lung cancer (NSCLC) patients harboring MET alterations, including those with brain metastases. The drug has been approved for use in China (2023) and Japan (2024) for the treatment of unresectable, advanced or recurrent NSCLC with MET exon 14 skipping mutations[10][7][3][6].

Brand names
谷美替尼
Other names
6-(1-methyl-1h-pyrazol-4-yl)-1-((6-(1-methyl-1h-pyrazol-4-yl)imidazo(1,2-a)pyridin-3-yl)sulfonyl)-1h-pyrazolo(4,3-b)pyridine
02

Targets

MET (Mesenchymal-epithelial transition factor receptor)

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