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

Abstract

AIMS:

This randomized, double-blind, placebo-controlled, parallel-group study evaluated the safety and efficacy of ezetimibe 10 mg/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) > or =3.36 mmol/l (130 mg/dl) to < or =6.47 mmol/l (250 mg/dl) and triglycerides < or =3.95 mmol/l (350 mg/dl) were randomized 3:1 to receive ezetimibe 10 mg 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 (P<0.01). Response to ezetimibe was generally consistent across all subgroups analyzed. Ezetimibe also significantly improved levels of plasma total cholesterol, apolipoprotein B, high-density lipoprotein(2)-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.

• Authors: R H Knopp, H Gitter, T Truitt, H Bays, C V Manion, L J Lipka, A P LeBeaut, R Suresh, B Yang, E P Veltri, Ezetimibe Study Group
• Journal: European heart journal (Eur Heart J) Vol. 24 Issue 8 Pg. 729-41 (Apr 2003) ISSN: 0195-668X [Print] England
• PMID: 12713767 (Publication Type: Clinical Trial, Journal Article, Multicenter Study, Randomized Controlled Trial)

Chemical References

• Anticholesteremic Agents
• Azetidines
• Cholesterol, LDL
• Triglycerides
• Vitamins
• Cosyntropin
• Ezetimibe

Topics

• Adult
• Aged
• Anticholesteremic Agents (therapeutic use)
• Azetidines (therapeutic use)
• Cholesterol, LDL (blood)
• Cosyntropin (blood)
• Double-Blind Method
• Ezetimibe
• Female
• Humans
• Hypercholesterolemia (blood, drug therapy)
• Male
• Middle Aged
• Single-Blind Method
• Triglycerides (blood)
• Vitamins (blood)