regorafenib + cetuximab

Regorafenib + cetuximab is an investigational combination regimen integrating a small molecule multikinase inhibitor (**regorafenib**) and a monoclonal antibody inhibitor of epidermal growth factor receptor (**cetuximab**), primarily studied for advanced and refractory **colorectal cancer**. Regorafenib blocks multiple kinases involved in angiogenesis, oncogenesis, and the tumor microenvironment, chiefly inhibiting **VEGF receptors 1–3, KIT, PDGFR-α/β, RET, FGFR1/2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, SAPK-2, PTK5, ABL**. Cetuximab binds to **EGFR**, blocking ligand-induced receptor activation and downstream signaling that drives tumor proliferation and survival. The combination is postulated to **overcome intrinsic and acquired resistance** in colorectal cancer by **simultaneous blockade of EGFR and VEGF pathways**, which often underpins resistance to single-agent therapy, with additional antitumor effects by blocking MAPK and AKT pathways and remodeling the tumor microenvironment.

Other names

regorafenibcetuximab