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.[1]
orally available, potent and highly selective inhibitor of nicotinamide phosphoribosyltransferase (NAMPT)
Molecular cancer therapeutics, 16(12), 2677-2688 (2017-10-22)
NAMPT, an enzyme essential for NAD+ biosynthesis, has been extensively studied as an anticancer target for developing potential novel therapeutics. Several NAMPT inhibitors have been discovered, some of which have been subjected to clinical investigations. Yet, the on-target hematological and
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