Ezetimibe: cholesterol lowering and beyond

Bays, Harold; Neff, David; Tomassini, Joanne E.; Tershakovec, Andrew M.

doi:10.1586/14779072.6.4.447

Cited by 135 publications

(90 citation statements)

References 134 publications

(185 reference statements)

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“…Trials that evaluate the lipid‐lowering efficacy of different modes of therapy may provide helpful information for physicians when considering therapeutic options for high‐risk patients on statin therapy in need of additional LDL‐C lowering. A number of studies have reported that combination ezetimibe/simvastatin (ES) therapy reduces LDL‐C and improves other lipids more than do statin monotherapy and doubling the statin dose or switching to a more‐potent statin, across a range of commonly prescribed doses in high‐risk patients including those with type 2 diabetes 17, 18, 19, 20. The recently completed IMPROVE‐IT trial (IMProved Reduction of Outcomes: Vytorin Efficacy International Trial) assessed the incremental cardiovascular benefit of LDL‐C lowering with ezetimibe 10 mg added to simvastatin (mainly 40 mg) compared with simvastatin monotherapy in patients presenting with acute coronary syndromes 21, 22, 23.…”

Section: Introductionmentioning

confidence: 99%

Effect of Switching From Statin Monotherapy to Ezetimibe/Simvastatin Combination Therapy Compared With Other Intensified Lipid‐Lowering Strategies on Lipoprotein Subclasses in Diabetic Patients With Symptomatic Cardiovascular Disease

Tomassini

Tershakovec

et al. 2015

JAHA

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BackgroundPatients with diabetes mellitus and cardiovascular disease may not achieve adequate low‐density lipoprotein cholesterol (LDL‐C) lowering on statin monotherapy, attributed partly to atherogenic dyslipidemia. More intensive LDL‐C–lowering therapy can be considered for these patients. A previous randomized, controlled study demonstrated greater LDL‐C lowering in diabetic patients with symptomatic cardiovascular disease who switched from simvastatin 20 mg (S20) or atorvastatin 10 mg (A10) to combination ezetimibe/simvastatin 10/20 mg (ES10/20) therapy, compared with statin dose‐doubling (to S40 or A20) or switching to rosuvastatin 10 mg (R10). The effect of these regimens on novel biomarkers of atherogenic dyslipidemia (low‐ and high‐density lipoprotein particle number and lipoprotein‐associated phospholipase A2 [Lp‐PLA2]) was assessed.Methods and ResultsTreatment effects on low‐ and high‐density lipoprotein particle number (by NMR) and Lp‐PLA2 (by ELISA) were evaluated using plasma samples available from 358 subjects in the study. Switching to ES10/20 reduced low‐density lipoprotein‐particle number numerically more than did statin dose‐doubling and was comparable with R10 (−133.3, −94.4, and −56.3 nmol/L, respectively; P>0.05). Increases in high‐density lipoprotein particle number were significantly greater with switches to ES10/20 versus statin dose‐doubling (1.5 and −0.5 μmol/L; P<0.05) and comparable with R10 (0.7 μmol/L; P>0.05). Percentages of patients attaining low‐density lipoprotein particle number levels <990 nmol/L were 62.4% for ES10/20, 54.1% for statin dose‐doubling, and 57.0% for R10. Switching to ES10/20 reduced Lp‐PLA2 activity significantly more than did statin dose‐doubling (−28.0 versus −3.8 nmol/min per mL, P<0.05) and was comparable with R10 (−28.0 versus −18.6 nmol/min per mL; P>0.05); effects on Lp‐PLA2 concentration were modest.ConclusionsIn diabetic patients with dyslipidemia, switching from statins to combination ES10/20 therapy generally improved lipoprotein subclass profile and Lp‐PLA2 activity more than did statin dose‐doubling and was comparable with R10, consistent with its lipid effects.Clinical Trial RegistrationURL: http://www.clinicaltrials.gov. Unique identifier: NCT00862251.

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Section: Introductionmentioning

confidence: 99%

Effect of Switching From Statin Monotherapy to Ezetimibe/Simvastatin Combination Therapy Compared With Other Intensified Lipid‐Lowering Strategies on Lipoprotein Subclasses in Diabetic Patients With Symptomatic Cardiovascular Disease

Tomassini

Tershakovec

et al. 2015

JAHA

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“…Among them, statins are recognized as the main cholesterol-lowering drugs by reducing the cholesterol contents through the inhibition of the 3-hydroxy-3-methyl-glutaryl coA reductase (HMGCR), an enzyme with a key function in the endogenous biosynthesis of the cholesterol 7 . On the other hand, ezetimibe also reduces cholesterol contents by interacting with the Niemann-Pick C1-like 1 (NPC1L1), which results in a decreased cholesterol absorption 8 . In addition, a number of pleiotropic effects have been described for statin therapy, including anti-inflammatory properties related to the vascular endothelium function 9 .…”

Section: Introductionmentioning

confidence: 99%

Role of Micro-RNAs 221/222 on Statin Induced Nitric Oxide Release in Human Endothelial Cells

Fajardo¹

2013

J Pharmacogenomics Pharmacoproteomics

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“…In several countries, therapeutic interventions that included various absorbable drugs with the purpose of reducing and of treating risk factors, particularly hypercholesterolemia, significantly lowered mortality due to cardiovascular disease (CVD) (3). More recently, inhibitors of the intestinal absorption of cholesterol such as ezetimibe have been used (4). Despite these therapeutic advances, ezetimibe has not been shown to be effective in human atherosclerosis (5).…”

Section: Introductionmentioning

confidence: 99%

Do clinical and experimental investigations support an antiatherogenic role for dietary phytosterols/stanols?

et al. 2012

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SummaryThe plasma cholesterol-reducing effect of phytosterols (PS) has been recognized in several studies, but the usefulness of PS in preventing coronary heart disease remains controversial, as some investigations claim that the high PS concentrations found in plasma and specific tissues are related to an increased risk of cardiovascular events. It has also been demonstrated that PS may induce inflammation and reduce cholesterol efflux from macrophages, conditions that are directly implicated in the development of atherosclerosis. As to arterial dysfunction and atherosclerosis, some studies have concluded that plasma PS concentrations are unrelated or only weakly related or that PS intake or plasma PS concentrations are harmful. Thus, in light of the National Cholesterol Education Program-ATPIII report, it is necessary to evaluate the relevance of their findings. To this end, we have evaluated the studies conducted on cells, animal models, and humans regarding the influence of PS on the development of atherosclerosis.2012 IUBMB IUBMB Life, 64(4): [296][297][298][299][300][301][302][303][304][305][306] 2012

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Ezetimibe: cholesterol lowering and beyond

Cited by 135 publications

References 134 publications

Effect of Switching From Statin Monotherapy to Ezetimibe/Simvastatin Combination Therapy Compared With Other Intensified Lipid‐Lowering Strategies on Lipoprotein Subclasses in Diabetic Patients With Symptomatic Cardiovascular Disease

Effect of Switching From Statin Monotherapy to Ezetimibe/Simvastatin Combination Therapy Compared With Other Intensified Lipid‐Lowering Strategies on Lipoprotein Subclasses in Diabetic Patients With Symptomatic Cardiovascular Disease

Role of Micro-RNAs 221/222 on Statin Induced Nitric Oxide Release in Human Endothelial Cells

Do clinical and experimental investigations support an antiatherogenic role for dietary phytosterols/stanols?

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