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Gumarontinib (also known as glumetinib or SCC-244) is an oral, potent, and highly selective small-molecule inhibitor of the mesenchymal-epithelial transition (MET) receptor tyrosine kinase. Co-developed by the Shanghai Institute of Materia Medica (SIMM) and Haihe Biopharma, gumarontinib is designed to target MET alterations, such as MET exon 14 skipping mutations and MET protein overexpression, which act as key oncogenic drivers in non-small cell lung cancer (NSCLC). It has demonstrated robust antitumor activity, a favorable pharmacokinetic profile with a long half-life allowing for once-daily dosing, and blood-brain barrier penetration, making it effective against central nervous system metastases. Gumarontinib received conditional approval in China in March 2023 and full approval in Japan in June 2024 for the treatment of advanced or recurrent MET-mutant NSCLC.
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