Tepotinib is a tyrosine kinase inhibitor targeting MET exon 14 skipping mutations, mainly used for the treatment of patients with advanced or metastatic non‑small cell lung cancer (NSCLC) harboring this gene mutation. It blocks the MET signaling pathway to inhibit tumor cell proliferation and metastasis, representing an important advance in precision medicine.
Mechanism of Action and Indications
Mechanism of Action
Tepotinib selectively binds to the MET protein and blocks its abnormal activation, thereby inhibiting downstream oncogenic signaling (including the RAS‑MAPK and PI3K‑AKT pathways).
Indications
Approved for adult patients with NSCLC confirmed to have MET exon 14 skipping mutations by molecular testing, especially for advanced cases in which first‑line therapy has failed or chemotherapy is not tolerated.
Clinical Efficacy
Clinical trials show that the objective response rate (ORR) of tepotinib in patients with MET mutations reaches 40%–50%, with a median duration of response (DOR) of approximately one year.
Common Side Effects
Common adverse reactions include peripheral edema, nausea, diarrhea, and fatigue, most of which are mild to moderate.Serious adverse reactions such as interstitial lung disease (ILD) and hepatotoxicity require close monitoring.
Precautions for Use
Genetic Testing
Molecular testing (such as NGS or PCR) is mandatory to confirm the MET mutation status before treatment initiation.
Dose Adjustment
Dose reduction or treatment interruption may be required based on the severity of adverse reactions, under strict medical supervision.
Drug Interactions
Avoid concomitant use with strong CYP3A inhibitors or inducers, which may alter plasma drug concentrations.
Patient Management Recommendations
Regular Monitoring
During treatment, periodic monitoring of liver function, electrolytes, and chest imaging is required to detect and manage adverse reactions promptly.
Lifestyle
A low‑salt diet helps alleviate edema.Immediate medical attention is needed for dyspnea or persistent fever.
Tepotinib is a prescription drug and must be used strictly under the guidance of a physician. Patients must not adjust the dose or discontinue treatment without authorization.
