Fatty acid synthase inhibitors: new directions for oncology

Expert Opin Investig Drugs. 2007 Nov;16(11):1817-29. doi: 10.1517/13543784.16.11.1817.


Fatty acid synthase (FASN) is the enzyme that catalyzes the de novo synthesis of fatty acids in cells. Because of the strong expression in many cancers, FASN is an attractive and tractable target for therapeutic intervention. The discovery and development of pharmacologic agents that block FASN activity highlight the promise of these anticancer compounds. FASN inhibitors have also proven to be invaluable in developing a better understanding of the contribution of FASN and fatty acid synthesis to tumor cells. Recent advances in the development of crystal structures of FASN have provided promise towards the development of novel FASN inhibitors. This review outlines the preclinical development of FASN inhibitors, their antitumor effects and the strategies underway to develop novel inhibitors.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use*
  • Cell Death / drug effects
  • Drug Design
  • Fatty Acid Synthases / antagonists & inhibitors*
  • Fatty Acid Synthases / metabolism
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism


  • Antineoplastic Agents
  • Fatty Acid Synthases