What target does capmatinib treat?

The primary target of capmatinib is the MET (mesenchymal epidermal transforming factor) tyrosine kinase receptor. METThe signaling pathway plays a key role in a variety of cellular functions, including cell growth, migration, survival, and angiogenesis. However, when the MET gene is mutated or amplified, it will trigger abnormal signal activation, thereby promoting the proliferation and metastasis of cancer cells. Capmatinib achieves the effect of treating cancer by precisely inhibiting MET kinase activity and blocking related signaling pathways.

Capmatinib mainly targets **METexon14 skipping mutation (METex14 skipping mutation) ** non-small cell lung cancer (NSCLC). This mutation will lead to overexpression or enhanced function of MET protein, disrupting normal cell regulatory mechanisms, and ultimately leading to the occurrence and development of cancer. METex14Skipping mutations account for about 3%-4% of NSCLC patients. They have poor response to traditional chemotherapy and immunotherapy, so targeted drug therapy is needed.

In addition toMETex14jumping mutations, capmatinib also shows certain efficacy against certain METamplification (MET amplification) and overexpression tumors. Under these circumstances, the abnormal activity of the MET signaling pathway will give cancer cells stronger invasion and drug resistance capabilities. Capmatinib provides a new treatment method by selectively inhibiting these abnormal signals.

Capmatinib binds to METtyrosine kinase and inhibits its kinase activity, thereby blocking downstream signaling pathways related to MET, such as PI3K/AKT and RAS/MAPK. These signaling pathways are critical in cell proliferation and survival. By inhibiting the excessive activation of these signaling pathways, capmatinib effectively reduces the proliferation, migration, and angiogenesis of cancer cells while inducing apoptosis.

Capmatinib, as the first approved MET inhibitor, fills the gap in the treatment of METex14 skipping mutation tumors. Its precise targeted therapy offers new hope for such patients and has shown high overall response rates and durable responses in clinical trials. At the same time, studies have also shown that capmatinib also has certain efficacy in some patients with MET amplification or overexpression, indicating that its scope of application may be further expanded.

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Reference materials

Official website of Novartis: https://www.novartis.com