Medicinal chemistry of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors

J Med Chem. 2013 Aug 22;56(16):6279-96. doi: 10.1021/jm4001049. Epub 2013 May 31.


Nicotinamide phoshophoribosyltransferase (NAMPT) plays a key role in the replenishment of the NAD pool in cells. This in turn makes this enzyme an important player in bioenergetics and in the regulation of NAD-using enzymes, such as PARPs and sirtuins. Furthermore, there is now ample evidence that NAMPT is secreted and has a role as a cytokine. An important role of either the intracellular or extracellular form of NAMPT has been shown in cancer, inflammation, and metabolic diseases. The first NAMPT inhibitors (FK866 and CHS828) have already entered clinical trials, and a surge in interest in the synthesis of novel molecules has occurred. The present review summarizes the recent progress in this field.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Crystallography, X-Ray
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Models, Molecular
  • Nicotinamide Phosphoribosyltransferase / antagonists & inhibitors*
  • Structure-Activity Relationship


  • Enzyme Inhibitors
  • Nicotinamide Phosphoribosyltransferase