In conclusion, although most medical treatments ameliorate the biochemical features of Cushing's disease to a variable degree, they do not inhibit pituitary tumor growth. The identification of the retinoic acid and PPAR-γ receptors as potential therapeutic targets in pituitary corticotroph tumors provides novel therapeutic options in the management of Cushing's disease. Rosiglitazone, a potent TZD oral antidiabetic agent, differs structurally from pioglitazone and troglitazone, and has greater PPAR-γ-binding affinity and antihyperglycemic potency. Surveillance of more than 4500 patients show that rosiglitazone is a safe, effective mono- or combination therapy for patients with Type 2 diabetes, and unlike troglitazone, which has been associated with idiosyncratic hepatotoxicity, rosiglitazone is associated with a low incidence of liver abnormalities. Given abundant and selective PPAR-γ expression in corticotroph pituitary tumors, compared to normal pituitary tissue, the potential use of TZD in treating patients with Cushing's disease now requires validation in a controlled clinical trial. © 2004, Editrice Kurtis.