Peroxisome proliferator-activated receptor gamma (PPARgamma) belongs to a nuclear receptor superfamily which agonists were in clinical use for anti-diabetic therapy. Recent studies both in vivo and in vitro revealed that PPARgamma agonists have anti-atherosclerotic effects which is also demonstrated by a large clinical trial including PROactive study. One of the mechanisms for this effect is the activation of reverse cholesterol transport through the induction of ABCA1 transporter by PPARgamma agonists. The transporter exports cholesterol from macrophages migrating in the vasculature and inhibits the formation of foam cell which contains lipid droplet in the cytosol as cholesterol ester. Clinical application of PPARgamma agonists have beneficial effects by preventing the cardiovascular events in diabetic patients.