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.
LIST OF FIGURES
13 Figure 1: Mekinist in melanoma – SWOT analysis
14 Figure 2: Datamonitor Healthcare’s drug assessment summary of Mekinist for melanoma
15 Figure 3: Datamonitor Healthcare’s drug assessment summary of Mekinist for melanoma
17 Figure 4: Mekinist sales for melanoma across the US, Japan, and five major EU markets, by country, 2017–26
LIST OF TABLES
6 Table 1: Mekinist drug profile
8 Table 2: Mekinist pivotal trial data in melanoma
11 Table 3: Mekinist ongoing late-phase clinical trials in melanoma
18 Table 4: Mekinist sales for melanoma across the US, Japan, and five major EU markets, by country ($m), 2017–26
20 Table 5: Mekinist patient numbers for melanoma across the US, Japan, and five major EU markets, by country, 2017–26
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