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Objective To evaluate the effect of pitavastatin on high-density lipoprotein cholesterol (HDL-C) level and cholesterol efflux and antioxidative properties of HDL in patients with dyslipidemia and stable coronary disease. Methods The study population included 60 patients with stable coronary disease and dyslipidemia. They were randomly allocated to treatment by pitavastatin 2-4 mg per day or atorvastatin 10-20 mg per day and followed up for six months. The cholesterol efflux and activities of antioxidative enzymes paraoxonase-1 (PON-1) were evaluated before and after statins treatment. Results The effect of the 6-month treatment with pitavastatin on serum HDL-C level was significantly greater than that of atorvastatin (% change: pitavastatin 9.0% vs atorvastatin 1.8%, P＜0.01). HDL induced cholesterol efflux increased significantly after the 6- month treatment with pitavastatin while it not was affected by atorvastatin treatment. However, HDL-associated PON-1 in both pitavastatin group and atovastatin group all increased. The activity of PON-1 increased by 21% with pitavastatin and 24% with atorvastatin, while the activity of arylesterase increased by 18% with pitavastatin and 17% with atorvastatin (P＜0.001). Conclusions Pitavastatin elevates the HDL-C level, enhances the cholesterol efflux and antioxidative effect of HDL. Therefore, pitavastatin increases the amount of functional HDL without attenuating HDL quality.