Tepotinib belongs to the first generation of targeted therapy drugs

Tepotinib is a selective MET inhibitor for the treatment of patients with non-small cell lung cancer (NSCLC) carrying MET exon 14 skipping mutations (METex14). Strictly speaking, tepotinib is not classified according to the traditional EGFR-TKI classification method. Instead, it belongs to a new generation of MET targeted therapy drugs that specifically targets MET gene abnormalities. It can be considered a first- or second-generation MET inhibitor, but due to its unique mechanism of action, it is more accurately classified as a new, more specific and highly selective MET inhibitor.

The MET signaling pathway plays an important role in tumor growth, invasion, and drug resistance. In particular, MET exon 14 skipping mutations can lead to continuous activation of MET protein, allowing cancer cells to continue to grow and evade attack by the immune system. Tepotinib can precisely inhibit this abnormal signaling pathway, thereby inhibiting tumor growth. Compared with early non-selective MET inhibitors (such as crizotinib), tepotinib is more effective against METex14 mutations and reduces non-specific inhibition of other tyrosine kinases, thereby reducing the incidence of side effects.

In clinical studies, tepotinib has demonstrated good efficacy and safety. According to the results of the VISION study, patients with advanced NSCLC carrying METex14 mutations can achieve an objective response rate (ORR) of 40-50% after receiving tepotinib treatment, and their progression-free survival (PFS) is significantly prolonged. In addition, Tepotinib is well tolerated, with common side effects including peripheral edema, nausea, diarrhea, etc. Compared with traditional chemotherapy and some non-selective MET inhibitors, Tepotinib is safer.

Therefore, although tepotinib does not belong to the first, second or third generation EGFR-TKI in the strict sense, it can be classified as a new generation of highly selective MET inhibitors and has important clinical value in the treatment of METex14 mutated non-small cell lung cancer.

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