Literature DB >> 11558859

Effectiveness and tolerability of ezetimibe in patients with primary hypercholesterolemia: pooled analysis of two phase II studies.

H E Bays1, P B Moore, M A Drehobl, S Rosenblatt, P D Toth, C A Dujovne, R H Knopp, L J Lipka, A P Lebeaut, B Yang, L E Mellars, C Cuffie-Jackson, E P Veltri.   

Abstract

BACKGROUND: Ezetimibe (SCH 58235) is a novel cholesterol absorption inhibitor that selectively and potently blocks intestinal absorption of dietary and biliary cholesterol.
OBJECTIVE: Data from 2 multicenter, placebo-controlled, double-blind, randomized, parallel-group, 12-week studies of ezetimibe were pooled to evaluate the drug's effect on lipid parameters in patients with primary hypercholesterolemia.
METHODS: After dietary stabilization (National Cholesterol Education Program Step I diet or a stricter diet), washout of lipid-altering drugs, and a 6-week placebo lead-in period, patients with baseline plasma low-density lipoprotein cholesterol (LDL-C) levels > or = 130 and < or = 250 mg/dL and plasma triglyceride (TG) levels < or = 300 mg/dL were randomized to receive either ezetimibe 0.25, 1, 5, or 10 mg, or placebo administered once daily before the morning meal in study A (dose-response study) or ezetimibe 5 or 10 mg or placebo administered once daily before the morning meal or at bedtime in study B (dose-regimen study).
RESULTS: A total of 432 patients were included in this pooled analysis, 243 in study A and 189 in study B. The 5- and 10-mg doses of ezetimibe significantly reduced LDL-C levels by 15.7% and 18.5%, respectively (P < 0.01 vs placebo) and significantly increased high-density lipoprotein cholesterol (hDL-C) levels by 2.9% and 3.5%, respectively (P < 0.05 vs placebo). A reduction in plasma TG levels was observed (P = NS). With the 10-mg dose of ezetimibe, 67.8% of patients achieved > or = 15% reduction in plasma LDL-C levels, and 22.0% achieved > or = 25% reduction. With the 5-mg dose, 54.0% of patients achieved > or = 15% reduction in plasma LDL-C levels, and 15.3% achieved > or = 25% reduction. The decrease in plasma LDL-C levels was significantly greater with ezetimibe 10 mg compared with ezetimibe 5 mg (P < 0.05). Ezetimibe was well tolerated, with an adverse event profile similar to that of placebo.
CONCLUSIONS: In these two 12-week studies, ezetimibe significantly decreased plasma LDL-C levels and increased plasma HDL-C levels, with a tolerability profile similar to that of placebo.

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Year:  2001        PMID: 11558859     DOI: 10.1016/s0149-2918(01)80102-8

Source DB:  PubMed          Journal:  Clin Ther        ISSN: 0149-2918            Impact factor:   3.393


  64 in total

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Authors:  Margaret E Brousseau; Ernst J Schaefer
Journal:  Curr Atheroscler Rep       Date:  2002-09       Impact factor: 5.113

2.  Pharmacodynamic interaction between the new selective cholesterol absorption inhibitor ezetimibe and simvastatin.

Authors:  Teddy Kosoglou; Ingo Meyer; Enrico P Veltri; Paul Statkevich; Bo Yang; Yali Zhu; Lillian Mellars; Stephen E Maxwell; James E Patrick; David L Cutler; Vijay K Batra; Melton B Affrime
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3.  Is bigger better? An argument for very low starting doses.

Authors:  James P McCormack; G Michael Allan; Adil S Virani
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4.  The clinical effect and tolerability of ezetimibe in high-risk patients managed in a specialty cardiovascular risk reduction clinic.

Authors:  Glen J Pearson; Gordon A Francis; Jacques S Romney; Dawna M Gilchrist; Andrea Opgenorth; Gabor T Gyenes
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Review 5.  Mechanisms, significance and treatment of vascular dysfunction in type 2 diabetes mellitus: focus on lipid-regulating therapy.

Authors:  Richard J Woodman; Gerard T Chew; Gerald F Watts
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6.  Hepatic Niemann-Pick C1-like 1 regulates biliary cholesterol concentration and is a target of ezetimibe.

Authors:  Ryan E Temel; Weiqing Tang; Yinyan Ma; Lawrence L Rudel; Mark C Willingham; Yiannis A Ioannou; Joanna P Davies; Lisa-Mari Nilsson; Liqing Yu
Journal:  J Clin Invest       Date:  2007-07       Impact factor: 14.808

Review 7.  Treating hypercholesterolemia: looking forward.

Authors:  Antonio M Gotto
Journal:  Clin Cardiol       Date:  2003-01       Impact factor: 2.882

Review 8.  Therapy to reduce risk of coronary heart disease.

Authors:  Daniel J Rader
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9.  Ezetimibe impairs uptake of dietary cholesterol oxidation products and reduces alterations in hepatic cholesterol metabolism and antioxidant function in rats.

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Journal:  Lipids       Date:  2013-04-16       Impact factor: 1.880

Review 10.  Newer pharmaceutical agents to treat lipid disorders.

Authors:  Michael H Davidson
Journal:  Curr Cardiol Rep       Date:  2003-11       Impact factor: 2.931

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