Which medications in the drug class Antineoplastics, MEK Inhibitors are used in the treatment of Non-Small Cell Lung Cancer (NSCLC)?

Updated: Mar 10, 2021
  • Author: Winston W Tan, MD, FACP; Chief Editor: Nagla Abdel Karim, MD, PhD  more...
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Antineoplastics, MEK 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. [231]  Blockage of MEK protein may affect tumors with mutated Ras proteins or other proteins influenced by MAPK pathway. 

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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