E7130

E7130 is a novel synthetic anticancer agent belonging to the halichondrin class, structurally derived from the natural product norhalichondrin B originally isolated from marine sponges. Developed through a total synthesis approach by Eisai in collaboration with Harvard University’s Kishi group, E7130 is notable for its exceedingly complex chemical structure and was produced at scale for clinical trials. Mechanistically, E7130 acts as a microtubule dynamics inhibitor with antineoplastic activity distinct from other microtubule-targeting agents such as paclitaxel. In addition to direct cytotoxic effects on tumor cells, it exerts unique actions on the tumor microenvironment by suppressing cancer-associated fibroblasts (CAF), reducing TGFβ1 production in CAFs (but not cancer cells), promoting vascular remodeling (increasing CD31-positive endothelial cells and collagen IV), and potentially enhancing immune activation by alleviating hypoxia and disrupting stromal-cancer cell interactions. These combined effects may contribute to improved therapeutic outcomes in solid tumors[1][3][4][5][7].

Other names

halichondrin analogue E7130norhalichondrin B analogue