The Effect of CS-514 on Serum Lipids and Apolipoproteins in Hypercholesterolemic Subjects
- Noriaki Nakaya, MD;
- Yasuhiko Homma, MD;
- Hiromitsu Tamachi, MD;
- Hiroshi Shigematsu, MD;
- Yoshiya Hata, MD;
- Yuichiro Goto, MD
- From Tokai University Tokyo Hospital (Dr Nakaya) and the Department of Medicine, Keio University School of Medicine (Drs Shigematsu and Hata), Tokyo; Tokai University Ohiso Hospital, Ohiso, Japan (Dr Homma); and the First Department of Internal Medicine, Tokai University School of Medicine, Isehara, Japan (Drs Tamachi and Goto).
Abstract
CS-514 is a metabolic product of compactin and has a potent cholesterollowering effect in vitro and in animal studies by inhibiting 3-hydroxy-3-methylglutaryl—coenzyme A reductase. The efficacy and adverse effects of the agent were studied in 41 hypercholesterolemic subjects by administering daily doses of 5, 20, or 40 mg for four weeks under double-blind conditions. Mean total serum cholesterol level was reduced by 11.1% in the 5-mg group, 18.8% in the 20-mg group, and 25.3% in the 40-mg group. Marked reduction of total serum cholesterol level was also observed in heterozygous familial hypercholesterolemics. Mean low-density lipoprotein cholesterol level and apolipoprotein B concentration decreased by 38.5% and 28.8%, respectively, in the 40-mg group, while high-density lipoprotein cholesterol level increased by 11.8%. No serious clinical and laboratory abnormalities were observed. Plasma cortisol and testosterone levels were not significantly affected. These results suggest that CS-514 will be a useful agent in the treatment of nonfamilial and heterozygous familial hypercholesterolemia.
(JAMA 1987;257:3088-3093)
Footnotes
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Reprint requests to Tokai University Tokyo Hospital, 1-2-5 Yoyogi, Shibuya-ku Tokyo 151, Japan (Dr Nakaya).
