A new dawn for the use of thiazolidinediones in cancer therapy

The thiazolidinedione (TZD) class of PPAR-γ ligands is predominantly known for its insulin sensitization activity. Unfortunately, these drugs have discernible side effects at diabetic dose. However, rosiglitazone and pioglitazone are still in the market with controversies. Past few years have noted the use of these drugs for the treatment of various other ailments.

In this review, the authors present the anticancer mechanisms of established TZDs and highlight some of the new-fangled agents discovered. Remarkable preclinical and clinical activity of the known and newly developed agents, alone or in combination with the known cytotoxic agents, offer a new perspective for clinical studies carving a niche in cancer chemotherapy.

Various preclinical and clinical studies strongly suggest a role for TZDs both alone and in combination with existing chemotherapeutic agents, for the treatment of cancer. The exploration of newer TZDs at different doses, as well as developing partial agonists, can potentially help in unveiling the underlying mechanisms of these therapeutics, and consequently, treat this dreadful group of diseases.