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Background: Hyperlipidemia is common in renal transplant recipients. The aim of the study was to evaluate the efficacy and safety of ezetimibe on lipid profile and renal function in renal transplant recipients. Methods: This prospective clinical trial study was done in a private nephrology clinic in Iafahan on 450 renal transplant patients between 2006-2009 years. Based on inclusion criteria, 78 patients were selected and ezetimibe was added to their previous treatment regimen. Patients were placed in three groups: group E (ezetimibe alone), group ES (ezetimibe with statin) and group EG (ezetimibe with gemfibrozil). All of the patients were evaluated before and three and six months after intervention. Finding: Sixty one patients with mean age of 49 ± 12.3 years were studied. Triglyceride was reduced significantly three and six months after intervention in E and ES groups. Cholesterol was reduced significantly three and six months after intervention in all three groups. During the six-month study, no case of rejection was found. Glomerular filtration rate (GFR) in the three groups was increased but it was not statistically significant (P > 0.05). Conclusion: Ezetimibe alone, or in combination with statin or gemfibrozil, is a safe and effective drug in the treatment of hypercholestrolemic patients with kidney transplantation and alone, or in combination with statin, is a safe and effective drug in the treatment of hypertriglyceridemic patients with kidney transplantation.