OBJECTIVE: Intensive as compared to mild statin therapy has been proven to be superior in improving cardiovascular outcome, whereas the effects of intensive statin therapy on inflammation and lipoprotein biomarkers are not well defined. METHODS: This study assigned essential hypertensive patients with dyslipidemia to 6 months administration of mild (1 mg/day, n = 34) or intensive pitavastatin therapy (4 mg/day, n = 29), and various lipid and inflammation biomarkers were measured at baseline, and 3 and 6 months after the start of treatment. RESULTS: Both pitavastatin doses were well tolerated, and there were no serious treatment-related adverse events. After 6 months, significant improvements in total cholesterol, triglycerides, low-density lipoprotein (LDL-) cholesterol, LDL/high-density lipoprotein cholesterol (LDL/HDL), apolipoproteins B, C-II, and E, apolipoprotein-B/apolipoprotein-A-I (Apo B/Apo A-I), and malondialdehyde (MDA-) LDL were observed in both groups. Compared with the mild pitavastatin group, the intensive pitavastatin therapy showed significantly greater decreases in C reactive protein (F = 3.76, p<0.05), total cholesterol (F = 10.65), LDL-cholesterol (F = 23.37), LDL/HDL (F = 12.34), apolipoproteins B (F = 19.07) and E (F = 6.49), Apo B/Apo A-I (F = 13.26), and MDA-LDL (F = 5.76) (p<0.01, respectively). CONCLUSION: Intensive pitavastatin therapy may have a more favorable effect not only in decreasing LDL-cholesterol but also in pleiotropic benefits in terms of improvement of apolipoproteins, inflammation, or oxidation.