<p>Rosiglitazone, a member of the thiazolidinedione class of antidiabetic agents, improves glycemic control by improving insulin sensitivity. Rosiglitazone is a highly selective and potent agonist for the peroxisome proliferator-activated receptor gamma (PPAR-&gamma;). In humans, PPAR receptors are found in key target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-&gamma; nuclear receptors regulates the transcription of insulinresponsive genes involved in the control of glucose production, transport, and utilization. In addition, PPAR-&gamma;-responsive genes also participate in the regulation of fatty acid metabolism. Pharmacological studies in animal models indicate that Rosiglitazone improves sensitivity to insulin in muscle and adipose tissue and inhibits hepatic gluconeogenesis. Rosiglitazone maleate is not chemically or functionally related to the sulfonylureas, the biguanides, or the alpha glucosidase inhibitors.</p>