NCIt definition : A water-soluble prodrug of a pyridyl cyanoguanidine compound and an inhibitor of nicotinamide
phosphoribosyltransferase (NAMPT) with potential antineoplastic activity. Teglarinad
is rapidly converted in the bloodstream into an active compound through hydrolytic
cleavage of the carbonate ester bond. The activated form inhibits NAMPT, thereby inhibiting
nicotinamide adenine dinucleotide (NAD ) biosynthesis and induces a rapid decline
in intracellular NAD followed by ATP reduction. As NAD is essential for tumor cell
growth, inhibition of NAMPT induces tumor cell death. NAMPT is an essential enzyme
in the synthesis of NAD and is upregulated in some cancers.;
Semantic type(s)