Abstract
It has been shown that CS-500 is a specific inhibitor of 3-hydroxy-3-methylglutaryl CoA reductase. The inhibition constant, Ki, of this drug for the enzyme is very small, that is 1-10nM. From the value of Ki and the distribution of the drug, we expected that lower dose than generally employed would exert hypolipidemic effect.
After the treatment with CS-500 at doses of 3-15mg/day for 2-4 weeks, serum cholesterol levels were reduced but triglyceride levels were unchanged. A patient, who had suffered from anginal attacks several times per day, was given CS-500 15mg/day. Two weeks after, the anginal attacks disappeared and the improvement of EKG was observed.
These observation suggested that relatively low dose of CS-500 is able to bring about the improvement of ischemic changes on EKG as well as reduction of serum cholesterol.
