Denibulin is a novel antineoplastic agent. Denibulin selectively targets and reversibly binds to the colchicine-binding site on tubulin and inhibits microtubule assembly. This results in the disruption of the cytoskeleton of tumor endothelial cells, ultimately leading to cell cycle arrest, blockage of cell division and apoptosis. This causes inadequate blood flow to the tumor and eventually leads to a decrease in tumor cell proliferation. Denibulin hydrochloride had been in phase I clinical trials for the treatment of solid tumours. It was generally well tolerated and showed decrease in tumor vascular parameters. However, no recent development has been reported.