NCIt definition : An orally available inhibitor of both monomer and dimer forms of activating mutations
of the serine/threonine-protein kinase BRAF (B-raf) protein, including V600 BRAF mutations,
non-V600 BRAF mutations, and RAF fusions, with potential antineoplastic activity.
Upon administration, BRAF inhibitor BGB-3245 targets and binds to both monomeric and
dimeric forms of activating BRAF mutations and fusions. This may result in the inhibition
of BRAF-mediated signaling and inhibit proliferation in tumor cells expressing BRAF
mutations and fusions. BRAF belongs to the RAF family of serine/threonine protein
kinases and plays a role in regulating the mitogen-activated protein kinase (MAPK)/
extracellular signal-regulated kinase (ERK) signaling pathway, which is often dysregulated
in human cancers and plays a key role in tumor cell proliferation and survival. BRAF
mutations and fusions have been identified in a number of solid tumors and are drivers
of cancer growth.;