LSN3154567 is an orally available, potent and highly selective inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). LSN3154567 exhibits broad spectrum and potent anticancer activities without causing retinopathy in the rat. LSN3154567co-administration with nicotinic acid (NA) produces potent anti-tumor activity in tumor xenograft models without retinal and hematological toxicities.
LSN3154567 might be useful in developing a novel cancer therapeutic.