Background: It has been known that angiotensin II type 1 receptor blocker (ARB) attenuated neointimal formation and vascular smooth muscle cell proliferation, with a decrease in inflammation. Statins may contribute to the beneficial effects of ARB on vascular diseases. Objectives: The aim of this study was to evaluate the long-term clinical effects of combination of ARB and statin compared to combination of angiotensin converting enzyme inhibitor and statin in coronary artery disease (CAD) patients who underwent percutaneous coronary intervention (PCI). Methods: A total of 240 patients with CAD who underwent PCI between January 2004 and December 2004 were enrolled by prospective, randomized manner and we divided them into two groups: Group I (losartan 50mg and simvastatin 40mg, n=120) and Group II (ramipril 5mg and simvastatin 40mg, n=120). We compared major adverse cardiovascular events at 12-month follow-up. Results: Most of the enrolled patients had acute coronary syndrome (Group I: 85%, Group II: 88%). Stent implantation was done in 95% of the patients and we used drug-eluting stents in only one third of the patients. At 6-month after PCI, the levels of low-density lipoprotein cholesterol and high-sensitivity C-reactive protein were significantly decreased in both groups (Group I: 144짹34 to 98짹34 mg/dl, 1.5짹0.5 to 0.5짹0.4 mg/dl vs. Group II: 140짹30 to 95짹28 mg/dl, 1.3짹0.7 to 0.3짹0.2 mg/dl). Follow-up angiogram was performed in 67% in Group I and 69% in Group II. The incidences of restenosis and target lesion revascularization were not different significantly and there was no difference in in-stent late loss between both groups (Group I: 15%, 13%, 0.63짹0.40 mm vs. Group II: 14%, 12%, 0.61짹0.34 mm). There were no significant differences in the incidence of cardiac death, myocardial infarction, cerebrovascular accident, and bypass graft at 12-month clinical follow-up between both groups. The event-free survival rate at 1 year was 84% in Group I and 86% in Group II. Conclusion: The combination therapy of losartan and simvastatin has comparable results with the combination therapy of ramipril and simvastatin in CAD patients who underwent PCI.