MAP2K1 and cancer: Binimetinib is an oral, potent, selective, allosteric, small-molecule inhibitor of MEK1/2 and is approved in multiple countries in combination with encorafenib for the treatment of patients with unresectable or metastatic BRAF V600E or V600K mutation-positive melanoma.8,9 Inhibiting both basal and induced levels of ERK phosphorylation in numerous BRAF-mutated cancer cell lines (half maximal inhibitory concentration [IC50] values as low as 5 nM), binimetinib has nanomolar activity against purified MEK enzyme (IC50, 12 nM).