Therapeutic potential of thiazolidinediones as anticancer agents

Expert Opin Investig Drugs. 2003 Dec;12(12):1925-37. doi: 10.1517/13543784.12.12.1925.


Thiazolidinediones (TZDs) are synthetic ligands that activate the nuclear receptor peroxisome proliferator-activated receptor-gamma (PPAR-gamma). These compounds are widely used in the treatment of Type 2 diabetes. TZDs have antitumour activity in a wide variety of experimental cancer models, in vitro and in vivo, by affecting the cell cycle, induction of cell differentiation and apoptosis as well as by inhibiting tumour angiogenesis. These effects are mediated through both PPAR-gamma-dependent and -independent pathways depending on concentration and tumour cell type. Angiogenesis inhibition mechanisms of TZDs include directly inhibiting endothelial cell proliferation and migration as well as decreasing tumour cell vascular endothelial growth factor production. Further studies suggest that TZDs may be effective in prevention of certain cancers and in the treatment of cancer as adjuvant therapy.

Publication types

  • Review

MeSH terms

  • Angiogenesis Inhibitors / therapeutic use
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / adverse effects
  • Antineoplastic Agents / therapeutic use*
  • Clinical Trials as Topic
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Thiazoles / administration & dosage
  • Thiazoles / adverse effects
  • Thiazoles / therapeutic use*


  • Angiogenesis Inhibitors
  • Antineoplastic Agents
  • Thiazoles