valecobulin

Valecobulin (NOV120401, CKD-516) is an orally administered small molecule prodrug developed as a vascular-disrupting agent (VDA) for the treatment of advanced solid tumors. It is rapidly converted in vivo to its active form, S-516. The drug acts primarily as a **tubulin polymerization inhibitor** by binding to the colchicine site on tubulin, leading to disruption of established tumor vasculature and subsequent tumor hypoxia and necrosis. Preclinical studies demonstrated potent cytotoxicity against various cancer cell lines—including those overexpressing P-glycoprotein—and strong antitumor efficacy in animal models. Clinical development included phase I and II trials for advanced solid tumors and colorectal cancer; however, further development was discontinued after phase II due to unspecified reasons[2][5][7].

Other names

S-516S516S 516