Binimetinib

Definition

An orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity. Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. Inhibition of MEK1/2 prevents the activation of MEK1/2 dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling. This may eventually lead to an inhibition of tumor cell proliferation and an inhibition in production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types.

Also known as ARRY 162, ARRY 438162, ARRY-162, ARRY-438162, ARRY162, ARRY438162, BINIMETINIB, MEK 162, MEK-162, MEK162, Mektovi — per NCIT

Also identified as

• ATC L01EE03 per RXNORM
• NCIT NCIT:C84865 per NCIT
• SCTID 772095008 per RXNORM
• SCTID 772195005 per RXNORM
• UNII 181R97MR71 per RXNORM

Indications