NCIt 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.;