alpelisib + binimetinib

Alpelisib + binimetinib is an investigational combination of two oral small molecule targeted therapies: alpelisib, a selective inhibitor of phosphatidylinositol 3-kinase-alpha (PI3Kα), and binimetinib, an inhibitor of mitogen-activated protein kinase kinases 1 and 2 (MEK1/2). Both agents are approved individually for specific cancers—alpelisib for PIK3CA-mutated breast cancer and PIK3CA-related overgrowth syndromes, and binimetinib for BRAF-mutant melanoma in combination with encorafenib. The combination of alpelisib + binimetinib is being explored for synergistic antitumor activity, especially in cancers with dual pathway activation or resistance to single pathway inhibition, such as certain solid tumors with activation of the PI3K/AKT and MAPK/ERK pathways[1][2][4]. Developmental research is ongoing, particularly in melanoma, colorectal cancer, and other solid tumors.