NCIt definition : An orally bioavailable small-molecule inhibitor of p38 and Tie2 kinases with potential
antineoplastic, anti-inflammatory and antiangiogenic activities. Pexmetinib binds
to and inhibits the activities of p38 and Tie2 kinases, which may inhibit the production
of proinflammatory cytokines and may decrease tumor angiogenesis and tumor cell growth
and survival. p38 is a MAP kinase that is often upregulated in cancer cells, playing
a crucial part in the production of a variety of cytokines involved in inflammation
and cellular proliferation such as tumor necrosis factor (TNF) and interleukin (IL)-1
and -6. Tie2 is an endothelial cell specific receptor that is activated by angiopoietins,
growth factors required for angiogenesis. This agent has also been reported to inhibit
other kinases including vascular endothelial growth factor receptor (VEGFR2) and Src
tyrosine kinases.;