CS-514 is a competitive inhibitor of HMG-CoA reductase. The effect of this agent on serum lipids and lipoproteins was studied in 10 healthy normocholesterolemic male volunteers by giving 20 mg of CS-514 or placebo twice a day for 7 days under double-blind conditions. The mean total serum cholesterol level decreased by 18.6% in the CS-514 group, whereas it increased by 7.4% in the placebo group and the difference between the two groups was statistically significant (P less than 0.01). LDL cholesterol and LDL apo B values were reduced by 22.6% and 23.2%, respectively. Serum triglyceride level did not change significantly. No clinical or laboratory abnormalities were observed.

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