Copyright © 2003 by the European Society of Cardiology.
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Effects of ezetimibe, a new cholesterol absorption inhibitor, on plasma lipids in patients with primary hypercholesterolemia
a Division of Metabolism, Endocrinology & Nutrition, Northwest Lipid Research Clinic, 325 Ninth Avenue, Room 465, Box 359720, Seattle, WA 98104, USA
b Jersey Research Foundation, Inc., Linwood, NJ, USA
c Health Advance Institute, Melbourne, FL, USA
d L-MARC Research Center, Louisville, KY, USA
e Oklahoma Medical Research Foundation, Oklahoma City, OK, USA
f Schering-Plough Research Institute, Kenilworth, NJ, USA
* Corresponding author. Tel.: +1-206-341-4413; fax: +1-206-731-8536
E-mail address: rhknopp{at}u.washington.edu
Aims This randomized, double-blind, placebo-controlled, parallel-group study evaluated the safety and efficacy of ezetimibe 10mg/day in patients with primary hypercholesterolemia.
Methods and results Following dietary stabilization, a 2–12-week washout period, and a 4-week, single-blind, placebo lead-in period, 827 patients with baseline low-density lipoprotein cholesterol (LDL-C) 
3.36mmol/l (130mg/dl) to 
6.47mmol/l (250mg/dl) and triglycerides 3.95mmol/l (350mg/dl) were randomized 3:1 to receive ezetimibe 10mg or placebo orally once daily in the morning for 12 weeks. The primary efficacy endpoint was percentage reduction in direct plasma LDL-C. Ezetimibe reduced direct LDL-C by a mean of 17.7% from baseline to endpoint, compared with an increase of 0.8% with placebo 
. Response to ezetimibe was generally consistent across all subgroups analyzed. Ezetimibe also significantly improved levels of plasma total cholesterol, apolipoprotein B, high-density lipoprotein2-cholesterol and lipoprotein(a), and elicited a trend toward lower triglyceride levels. Ezetimibe did not alter the serum concentrations of lipid-soluble vitamins or significantly affect baseline or stimulated cortisol production. Ezetimibe was well tolerated, with a safety profile similar to that of placebo.
Conclusions Ezetimibe, which significantly reduces LDL-C and favorably affects other lipid variables, may provide a well tolerated and effective new option for lipid management in the future.
Key Words: Ezetimibe • Efficacy • Hypercholesterolaemia • Safety • Selective cholesterol absorption inhibitor
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