CHS-828

CHS-828 is a small molecule antineoplastic agent that acts as a potent and selective inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme in the biosynthesis of nicotinamide adenine dinucleotide (NAD). By inhibiting NAMPT, CHS-828 depletes cellular NAD levels, leading to cytotoxicity in tumor cells. This mechanism indirectly inhibits sirtuin enzymes and increases reactive oxygen species (ROS) selectively in cancer cells. Preclinical studies demonstrated antitumor activity both in vitro and in vivo. Clinical development included phase I trials for advanced solid tumors, where dose-limiting toxicities were primarily gastrointestinal symptoms and thrombocytopenia; no objective tumor remissions were observed[1][3][5][6][7][8].

Other names

N-[6-(4-chlorophenoxy)hexyl]-N'-cyano-N''-4-pyridinylguanidine