Triparanol, an inhibitor of cholesterol biosynthesis, significantly reduced the serum cholesterol in 71 of 89 subjects with and without hypercholesterolemia. The compound in a maximally effective dose of 250 mg. per day was well tolerated and caused no serious side effects. The decrease in serum cholesterol (Abell) averaged 45 mg. % and ranged from 20 to 110 mg. %. The ratio of serum cholesterol to serum phospholipid also was favorably influenced by therapy.
Triparanol, as indicated by radioisotopic tracer studies, also appeared to reduce the total sterol and cholesterol content of the body by decreasing the formation of cholesterol the body.
The compound appeared to have an anti-anginal effect in 12 of 28 subjects and to improve the electrocardiographic responses to exercise in 3 of 11 subjects with angina pectoris. These effects were associated with a fall in serum cholesterol.