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Daporinad is a highly selective, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT or NMPRTase), the rate-limiting enzyme in the biosynthesis of nicotinamide adenine dinucleotide (NAD+) from niacinamide (vitamin B3). By inhibiting NAMPT, daporinad depletes NAD+ levels in metabolically active tumor cells, leading to energy depletion and induction of tumor cell apoptosis. It may also inhibit tumor angiogenesis by reducing vascular endothelial growth factor (VEGF) production. Daporinad has been investigated primarily as an anti-cancer agent in clinical trials for B-cell chronic lymphocytic leukemia, melanoma, and cutaneous T-cell lymphoma. Clinical studies have shown low efficacy when used as monotherapy[1][2][4][5].
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