E7820 + cetuximab

E7820 is a small molecule, aromatic sulfonamide derivative developed as an oral angiogenesis inhibitor with potential antiangiogenic and antitumor activities. It acts primarily by inhibiting integrin alpha 2 (ITGA2), a cell adhesion molecule expressed on endothelial cells, thereby suppressing angiogenesis and tumor growth. Mechanistically, E7820 reduces integrin alpha 2 mRNA expression and has also been shown to act as a molecular glue that promotes the degradation of CAPERα via DCAF15-mediated ubiquitination, affecting RNA splicing and protein homeostasis in cancer cells. Cetuximab is a monoclonal antibody targeting the epidermal growth factor receptor (EGFR). The combination of E7820 with cetuximab has been investigated in clinical trials for advanced solid tumors, particularly colorectal cancer[1][4][5][6].

Other names

N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide3-cyano-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamideER-68203–00