Aim To explore the effect of ezetimibe on insulin release in unstable angina patients in prediabetes. Methods 222 unstable angina patients in prediabetes were randomly divided into control group and combined treatment group. In addition to routine treatment, control group was given atorvastatin 20 mg, while combined treatment group was given atorvastatin 20 mg and ezetimibe 10 mg. All patients were treated for 3 months. Oral glucose tolerance test (OGTT) and insulin release test (IRT) were examined at 7 d, 1 months, 3 months of medication. Results Compared with control group, blood glucose of OGTT on 0.5 h, 1 h, 2 h were significantly lower in combined treatment group at 7 d, 1 months, 3 months (P<0.5,0.01), and area under the curve (AUC) of blood glucose on 0.5 h, 1 h, 2 h, 3 h were significantly lower(P<0.5,0.1,0.001); insulin of IRT on 0.5 h, 1 h were significantly higher and insulin on 2 h were lower in combined treatment group at 7 d, 1 months, 3 months(P<0.5,0.01),and AUC of insulin on 0.5 h, 1 h, 2 h were significantly higher(P<0.1,0.1,0.05). AUC of blood glucose was negatively correlated with AUC of insulin (r=-0.387,P<0.01),and decrease of blood glucose was postively correlated with increase of insulin at different periods(r=0.473,P<0.001). Compared with control group, homeostasis model assessment (HOMA) for insulin resistance were significantly lower in combined treatment group at 1,3 months (P<0.5,0.01); insulin activity index at 7 d, 1 months, 3 months and HOMA-β at 3 months were significantly higher (P<0.5,0.01). Conclusion Ezetimibe can improve glucose tolerance by restored insulin release and increased insulin sensitivity on unstable angina patients in prediabetes.