The aim of this study was to compare the effects of 3 different statin regimens that have equivalent low-density lipoprotein cholesterol (LDL-C) lowering efficacy on the apolipoprotein B/A1 ratio and glucose metabolism. After a 4-week dietary lead-in, 90 hypercholeserolemic patients were randomly assigned to 1 of 3 treatment groups for 8 weeks: atorvastatin 20 mg, rosuvastatin 10 mg, or atorvastatin/ezetimibe 5 mg/5 mg. At drug treatment week 8, we compared the percentage changes in lipid parameters, apolipoprotein B/A1 ratio, hemoglobin A1c, and homeostasis model assessment-insulin resistance (HOMA-IR) from baseline. Seventy-six patients completed the study and the percentage changes in LDL-C were comparable among the groups. However, the percentage reduction in the apolipoprotein B/A1 ratio was significantly greater in the rosuvastatin group (-47% +/- 14%, P = .04) and the combination group (-46% +/- 8%, P = .05) than in the atorvastatin group (-39% +/- 11%). The percentage increase in hemoglobin A1c was small but significantly greater in the atorvastatin group compared to the combination group (3.0% +/- 5.2% and -0.4% +/- 4.0%, P = .03). The effect of rosuvastatin on hemoglobin A1c was not different from those of the other 2 regimens. The effects of 3 statin regimens were similar on HOMA-IR. In conclusion, 3 statin regimens have differential effect on apolipoprotein B/A1 and glycemic control after comparable LDL-C reduction.