Rapid and substantial lowering of human serum cholesterol by mevinolin (MK-803), an inhibitor of hydroxymethylglutaryl-coenzyme a reductase

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      Mevinolin (MK-803) is a potent inhibitor of HMG-CoA reductase. After a placebo run-in period, mevinolin 5, 15 or 50 mg, or placebo was given twice daily for 7–11 days under double-blind conditions to 4 groups of 6 normocholesterolemic male volunteers. After 7 days, mean serum cholesterol fell 14%, 25% and 24% on 5, 15 and 50 mg, respectively, which was significantly greater than the fall on placebo (4%) in the case of the two higher doses (P < 0.01). Serum triglycerides did not change significantly. Mevinolin was generally well tolerated and there were no serious adverse effects.


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