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**MLN2480 + cetuximab** is an investigational combination therapy consisting of MLN2480, a brain-penetrant, oral, type II pan-RAF kinase inhibitor (also known as TAK-580), and cetuximab, a chimeric monoclonal antibody targeting the epidermal growth factor receptor (EGFR). MLN2480 inhibits both monomeric and dimeric forms of BRAF by binding the inactive (DFG-out) conformation, blocking downstream MAPK pathway signaling, and is active against several BRAF mutants, with strong penetration of the blood-brain barrier[1][2][4]. Cetuximab binds to EGFR and inhibits ligand-induced receptor activation, blocking downstream signaling involved in cell proliferation and survival. The combination has been evaluated in phase 1 studies in patients with advanced solid tumors, particularly those failing standard therapies[7].
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