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LSN3154567 is a small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), an enzyme that serves as the rate-limiting step in the NAD+ salvage pathway. By inhibiting NAMPT, the compound depletes intracellular nicotinamide adenine dinucleotide (NAD+) levels, which are essential for cellular energy metabolism, DNA repair, and signaling. This depletion leads to metabolic collapse and induces apoptosis in cancer cells. Developed by Eli Lilly, LSN3154567 has been evaluated in large-scale pan-cancer screens where it demonstrated significant anti-proliferative activity across various malignancies, with particular sensitivity observed in acute myeloid leukemia (AML), ovarian cancer, Ewing's sarcoma, and small cell lung cancer (SCLC).
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