Which medications in the drug class MET Tyrosine Kinase Inhibitors are used in the treatment of Non-Small Cell Lung Cancer (NSCLC)?

Updated: Jul 15, 2021
  • Author: Winston W Tan, MD, FACP; Chief Editor: Nagla Abdel Karim, MD, PhD  more...
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MET Tyrosine Kinase Inhibitors

Mitogen extracellular signal-regulated kinase (MEK) protein acts downstream from Ras in the mitogen-activated protein kinase (MAPK) pathway. MAPK pathway regulates cell growth, cell differentiation, cell migration, and apoptosis. [233]  Blockage of MEK protein may affect tumors with mutated Ras proteins or other proteins influenced by MAPK pathway.

Capmatinib (Tabrecta)

Capmatinib is a kinase inhibitor that targets mesenchymal-epithelial transition (MET) , including the exon 14 skipping mutation. MET tyrosine kinase stimulates cell scattering, invasion, protection from apoptosis, and angiogenesis. A variety of cancers (eg, lung, gastric) are associated with dysregulation of MET, owing to MET amplifications and exon 14 skipping mutations. Capmatinib is indicated for metastatic NSCLC in adults whose tumors have a mutation that leads to exon 14 skipping.

Tepotinib (Tepmetko)

Tepotinib is an inhibitor of MET tyrosine kinase, which selectively binds to MET tyrosine kinase and disrupts MET signal transduction pathways. Therefore, this disruption may induce apoptosis in tumor cells overexpressing this kinase. It is indicated for metastatic NSCLC in patients with MET exon 14 skipping mutation.

Trametinib (Mekinist)

Trametinib is a selective reversible inhibitor of mitogen-activated extracellular signal regulated kinase 1 (MEK1) and MEK2 activation and kinase activity. Trametinib inhibits activation of MEK by BRAF and inhibits MEK kinase activity BRAF V600E mutations result in constitutive activation of the BRAF pathway, which includes MEK1 and MEK2. Trametinib inhibits cell growth in BRAF V600 mutation positive tumors in vitro and in vivo. It is indicated, in combination with dabrafenib, for the treatment of patients with metastatic NSCLC with BRAF V600E mutation as detected by an FDA-approved test.

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