Abstract: AIM:To explore the regulatory effect of ezetimibe combined with simvastatin on lipid and inflammatory cytokines in patients with coronary heart disease (CHD). METHODS: Sixty patients with CHD admitted to our hospital between May 2011 and September 2011 were randomly divided into two groups: treatment group and control group (30 patients/group). Ezetimibe (10 mg/day) combined with simvastatin (20 mg/day) was used in the treatment group and independent simvastatin (40 mg/day) was administered in the control group. Total cholesterol (TC), triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C), hepatic function, renal function, and creatine kinase (CK) were examined, respectively, before administration and 4 weeks and 8 weeks after administration. RESULTS: Compared with baseline level, TC and LDL-C decreased in the two groups 4 weeks after administration (P<0.05). After 8 weeks, these indicators decreased further in both groups (P<0.01). Compared with those in control group, TC and LDL-C in treatment group significantly decreased after 8 weeks (P<0.05). No significant differences of hepatic function, renal function and CK were found in both groups. CONCLUSION: Ezetimibe combined with simvastatin was shown to be more effective in decreasing serum lipid concentrations in patients with CHD.