sotrastaurin + binimetinib

Sotrastaurin + binimetinib is an investigational **combination regimen** of two oral small-molecule inhibitors: sotrastaurin, a selective inhibitor of classical and novel isoforms of protein kinase C (PKC), and binimetinib, a selective oral ATP-noncompetitive inhibitor of MEK1/2 (mitogen-activated protein kinase kinase). This combination was designed to concurrently block the PKC and MAPK/ERK signaling pathways, both of which are aberrantly activated in uveal melanoma, particularly those harboring GNAQ or GNA11 mutations. Preclinical studies demonstrated synergistic antitumor activity. The regimen underwent phase Ib clinical testing in metastatic uveal melanoma, with stable disease observed in most patients but no radiographic responses and substantial gastrointestinal toxicity. Further development for this indication was terminated due to limited efficacy and tolerability[1][3][5].

Brand names

Mektovi (for binimetinib; not a brand for the combination)

Other names

sotrastaurin + binimetinib