MET Targeting

Oncogenic Signaling

MET targeting

MET signaling is critical in normal biological processes. It activates downstream signaling pathways, including RAS/ERK/MAPK, PI3K/AKT, and JAK/STAT, which drive cell proliferation, motility, and apoptosis. Dysregulation of the MET pathway (for example MET mutations and amplifications) can drive cancer cell proliferation, survival, invasion, and metastasis.1

Tepotinib – MET kinase inhibitor

Tepotinib is a small-molecule inhibitor of the MET receptor tyrosine kinase. Alterations of the MET signaling pathway are found in various cancer types, and are thought to correlate with aggressive tumor behavior and poor clinical prognosis.1

VISION2 (NCT02864992)

A Phase 2 single-arm trial to investigate tepotinib in advanced (locally advanced or metastatic) non-small cell lung cancer with MET exon 14 skipping alterations or MET amplification.

INSIGHT 23 (NCT03940703)

A Phase 2 clinical trial to investigate tepotinib combined with osimertinib in patients with osimertinib-resistant, MET-amplified, EGFR-mutant NSCLC.

Targeting MET

Are you interested in learning more about a clinical trial program investigating the inhibition of oncogenic signaling caused by MET (gene) alterations?

The investigational compound combinations in the INSIGHT 2 trial are not approved by any health authority. Safety and efficacy have not been established.

AKT, protein kinase B; EGFR, epidermal growth factor receptor; ERK, extracellular signal-regulated kinase; JAK, Janus kinase; MAPK, mitogen-activated protein kinase; MET, mesenchymal epithelial transition factor; NSCLC, non-small cell lung cancer, PI3K; phosphatidylinositol 3 kinase; RAS; rat sarcoma, STAT; signal transducers and activators of transcription.

  1. Wu Y-L, Soo RA, Locatelli G, Stammberger U, Scagliotti G, Park K. Does c-Met remain a rational target for therapy in patients with EGFR TKI-resistant non-small cell lung cancer? Cancer Treat Rev. 2017;61:70-81.
  2. Tepotinib phase II in NSCLC harboring MET alterations (VISION). ClinicalTrials.gov identifier: NCT02864992. Updated December 1, 2023. Accessed December 1, 2023. https://www.clinicaltrials.gov/ct2/show/NCT02864992 
  3. A study of tepotinib plus osimertinib in osimertinib relapsed MET amplified NSCLC (INSIGHT 2). ClinicalTrials.gov identifier: NCT03940703. Updated November 30, 2023. Accessed December 1, 2023. https://www.clinicaltrials.gov/ct2/show/NCT03940703

GL-MULO-00164 | January 2024