Capmatinib (Touradida) belongs to which generation of targeted drugs and analysis of its clinical advantages

Capmatinib (trade name Tabrecta) is a selective MET tyrosine kinase inhibitor and is a second-generation targeted drug. Compared with the first-generation multi-target inhibitors, capmatinib is more targeted in molecular design and can efficiently and specifically inhibit tumor growth driven by MET gene exon 14 skipping mutations (METex14). The drug received accelerated approval from the US FDA in 2020 and is mainly used to treat patients with metastatic non-small cell lung cancer (NSCLC) with METex14 mutations.

Capmatinib has demonstrated a high objective response rate (ORR) in clinical trials, especially in first-line treatment, with its ORRIt can reach more than 60%, and some patients even achieve progression-free survival of more than one year (PFS). Its targeting effect is precisely focused on the MET signaling pathway, which can effectively block the proliferation and metastasis of tumor cells. Compared with traditional chemotherapy, the treatment response is faster and the side effects are more controllable, thereby improving the patient's quality of life.

Compared with some earlyMET inhibitors, capmatinib has good blood-brain barrier penetration ability, which gives it a clear advantage in NSCLC patients with brain metastases. Studies have shown that capmatinib can also produce significant tumor shrinkage effects in brain metastases, providing a new treatment option for this type of patients with poor prognosis. This feature is particularly important clinically because the treatment of lung cancer with brain metastasis has always been a problem.

Although capmatinib is effective, some patients may develop resistance due to secondary mutations or activation of bypass pathways after using it for a period of time. In the future, strategies combining other targeted drugs, immunotherapy or chemotherapy are expected to extend the duration of efficacy. In addition, more clinical trials of capmatinib in other MET abnormal driver tumors (such as gastric cancer, liver cancer) are also ongoing, which is expected to broaden its scope of indications. Taken together, capmatinib has become one of the important treatment options for METex14mutated NSCLC due to its precise targeting, high CNS activity and good tolerability.

Reference materials:https://www.drugs.com/