Capmatinib belongs to the first generation of targeted drugs

Capmatinib is an oral targeted drug targeting MET gene mutations and belongs to a new generation of selective MET inhibitors. It is different from the traditional first- and second-generation targeted drugs targeting EGFR, ALK, ROS1, etc., and is more accurately classified as a third-generation or new highly selective MET targeted therapy drug. It has shown important clinical value especially in the treatment of patients with MET gene exon 14 skipping mutation (METex14 skipping mutation) and MET amplification in non-small cell lung cancer (NSCLC).

The receptor tyrosine kinase encoded by the MET gene plays a key role in cell proliferation, migration, and invasion. Its mutation or amplification can lead to abnormal activation of signaling pathways and is a driver of various tumor types. Traditional targeted drugs often have broad effects and many side effects, while capmatinib has higher target specificity and the ability to precisely inhibit MET kinase activity. Therefore, it is regarded as an advanced representative in the field of MET targeted therapy.

From the perspective of drug research and development, capmatinib embodies the development trend of "precise positioning" of targeted drugs, that is, developing corresponding inhibitors based on different molecular mutations. Compared with early multi-target tyrosine kinase inhibitors, it has relatively fewer side effects, is better tolerated, and has more clinical therapeutic value for specific groups of people, such as patients with MET mutations.

In 2020, capmatinib was approved by the US FDA for the treatment of metastatic non-small cell lung cancer carrying METex14 mutations. It is the world's first MET inhibitor approved to treat such gene mutations, which is a milestone. Therefore, although the definition of its "generation" is not completely unified in the academic community, it is recognized as a new generation of highly selective, modern molecular target drugs and an important part of precision medicine.

Reference materials:https://www.drugs.com/mtm/capmatinib.html