Tepotinib

(Tepmetko®)

Tepmetko®

Drug updated on 10/25/2024

Dosage FormTablet (oral; 225 mg)
Drug ClassKinase inhibitors
Ongoing and
Completed Studies
ClinicalTrials.gov

Indication

  • Indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) harboring mesenchymal-epithelial transition (MET) exon 14 skipping alterations.

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Summary
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  • This summary is based on the review of four systematic review(s)/meta-analysis(es). [1-4]
  • Tepotinib demonstrated an objective response rate (ORR) of 44.7% and a disease control rate (DCR) of 69.1% in patients with MET (METex14)-altered non-small cell lung cancer (NSCLC). In specific subgroups, patients with MET exon 14 skipping showed an ORR of 39.3%, and those with intracranial disease had an intracranial response rate of 40.1%.
  • Comparative Effectiveness: Tepotinib had a higher ORR (44.7%) compared to other MET inhibitors with a pooled ORR of 28.1%. Targeted MET tyrosine kinase inhibitors (TKIs), including tepotinib, showed superior efficacy (ORR of 50.7%-68.8%) compared to chemotherapy (23.1%-27.0%) and immunotherapy (33.3%) in METex14 skipping NSCLC.
  • Subgroup Considerations: Tepotinib was particularly effective in NSCLC patients with exon 14 skipping and those with intracranial metastases, offering higher response rates and disease control compared to other therapies, making it a preferred option in these genetic subgroups.
  • In patients treated with tepotinib, 87.2% experienced mild adverse events (grade 1 to 2). The most common grade 3 or higher adverse events were lower extremity edema (3.5%), alanine aminotransferase (ALT) elevation (2.4%), and lipase elevation (2.2%).
  • The safety profile of tepotinib, when compared with other MET inhibitors, was favorable, with mostly mild adverse events and a low incidence of severe adverse reactions. There were no significant safety concerns highlighted for specific populations or subgroups.
  • These findings are clinically relevant, especially in elderly patients, who are more likely to have MET exon 14 skipping mutations, and in histological subtypes like sarcomatoid (12% frequency of MET exon 14 skipping).