Drug Overview
Mekinist (trametinib; Novartis/Japan Tobacco) is a selective allosteric inhibitor of the MEK1 and MEK2 enzymes in the mitogen-activated protein kinase (MAPK) pathway. MEK1 and MEK2 are dual-specificity protein kinases that exist downstream of BRAF in the MAPK pathway. This close relationship with BRAF in the MAPK pathway has made MEK an attractive target to drug developers. MEK only has one known substrate, ERK, which could make MEK inhibitors more effective as there is potential to limit the chance of alternative pathways activating proliferation and survival (Dhomen and Marais, 2009). The majority of cells expressing a BRAF mutation are dependent on MEK activity and are therefore sensitive to MEK inhibition.
Mekinist (trametinib; Novartis/Japan Tobacco) is a selective allosteric inhibitor of the MEK1 and MEK2 enzymes in the mitogen-activated protein kinase (MAPK) pathway. MEK1 and MEK2 are dual-specificity protein kinases that exist downstream of BRAF in the MAPK pathway. This close relationship with BRAF in the MAPK pathway has made MEK an attractive target to drug developers. MEK only has one known substrate, ERK, which could make MEK inhibitors more effective as there is potential to limit the chance of alternative pathways activating proliferation and survival (Dhomen and Marais, 2009). The majority of cells expressing a BRAF mutation are dependent on MEK activity and are therefore sensitive to MEK inhibition.
Table of Contents
OVERVIEW
LIST OF FIGURES
LIST OF TABLES
