Pioglitazone is an oral antidiabetic agent that decreases insulin resistance in adipose tissue, liver and muscles. This action is mediated by its link to a nuclear receptor called peroxisome proliferator-activated receptor-gamma. By improving insulin sensitivity, hepatic glucose production decreases and glucose uptake increases in the peripheral tissues. Beyond these effects on glucose metabolism, pioglitazone has positive effects on lipid metabolism, blood pressure, endothelial function, adiponectin and C-reactive protein levels. These make pioglitazone treatment effective beyond glucose control. In this article, current evidence concerning pioglitazone in the treatment of Type 2 diabetes will be reviewed.