European Heart Journal

European Heart Journal 2003 24(8):729-741; doi:10.1016/S0195-668X(02)00807-2
Copyright © 2003 by the European Society of Cardiology.

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Regular Articles

Effects of ezetimibe, a new cholesterol absorption inhibitor, on plasma lipids in patients with primary hypercholesterolemia

R.H. Knopp^a,*, H. Gitter^b, T. Truitt^c, H. Bays^d, C.V. Manion^e, L.J. Lipka^f, A.P. LeBeaut^f, R. Suresh^f, B. Yang^f and E.P. Veltri^f for the Ezetimibe Study Group

^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

	Abstract

Top Abstract 1. Introduction 2. Materials and methods 3. Results 4. Discussion 5. Conclusions Appendix A: >The Ezetimibe... References

 
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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	Acknowledgments

 
The authors wish to thank Arlene Reiss for her assistance in the preparation of this manuscript.

	Footnotes

 
Deceased.

	References

Top Abstract 1. Introduction 2. Materials and methods 3. Results 4. Discussion 5. Conclusions Appendix A: >The Ezetimibe... References

 

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