NAMPT Inhibitor RPT1G

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable hyperbolic inhibitor of the nicotinamide adenine dinucleotide (NAD)-synthesizing enzyme nicotinamide phosphoribosyltransferase (NAMPT; NAMPRTase), with potential antineoplastic activity. Upon oral administration, NAMPT inhibitor RPT1G targets, binds to, and partially and reversibly inhibits the activity of NAMPT. This decreases cellular NAD supply and inhibits NAD-dependent enzymes, both of which are needed for rapid cell proliferation, which may result in cell death in NAMPT-overexpressing tumor cells. NAMPT, an enzyme that is responsible for maintaining the intracellular NAD pool, plays a key role in the regulation of cellular metabolism and has cytokine-like activities. NAMPT is overexpressed in a variety of cancers and metabolic disorders; tumor cells rely on NAMPT activity for their NAD supply. The partial and reversible inhibition of NAMPT may reduce on-target, dose-limiting toxicities as healthy tissues also depend on NAD for survival.

**Synonyms:** - NAMPT Hyperbolic Inhibitor RPT1G - NAMPTi RPT1G - Nicotinamide Phosphoribosyltransferase Inhibitor RPT1G - RPT 1G - RPT-1G - RPT1G