BI-847325

BI-847325 is an orally bioavailable, ATP-competitive dual inhibitor of MEK (MAP2K1/2) and Aurora kinases (AURKA/B, pan-Aurora) developed for cancer therapy, showing antitumor activity across multiple solid and hematologic tumor models in vitro and in vivo and inducing regression in several xenografts, including BRAF-mutant melanoma and colorectal models.[1][5][3] In a first-in-human phase 1 study in refractory solid tumors, BI-847325 demonstrated an acceptable safety profile but insufficient MEK inhibition at the maximum tolerated dose, leading to discontinuation of its clinical development.[2] Mechanistically, BI-847325 inhibits MEK/ERK phosphorylation and Aurora B–dependent histone H3 phosphorylation, decreases MEK and Mcl-1 expression, and increases pro-apoptotic BIM, consistent with dual MAPK pathway suppression and mitotic disruption.[1][5]

Other names

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