Efficacy and safety of ezetimibe added to ongoing statin therapy for treatment of patients with primary hypercholesterolemia

Gagné, Claude; Bays, Harold; Weiss, Stuart; Mata, Pedro; Quinto, Katherine; Melino, Michael; Cho, Meehyung; Musliner, Thomas; Gumbiner, Barry M.

doi:10.1016/s0002-9149(02)02774-1

Cited by 459 publications

(280 citation statements)

References 13 publications

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“…40,46,47 Together, these data clearly demonstrate that the dual inhibition of both cholesterol synthesis and absorption is an attractive new strategy for the treatment of primary hypercholesterolemia.…”

Section: Efficacy Of Combination Therapy Using Ezetimibe With a Statinmentioning

confidence: 79%

“…Ezetimibe blocks the absorption of cholesterol and plant sterols, but does not affect the absorption of bile acids, fatty acids, fat soluble vitamins, or triglycerides. 40,41 Newly published studies show that ezetimibe reduces cholesterol absorption by inhibiting a pathway in the brush border membrane of the enterocytes that is dependent on the activity of NPC1L1. 13 …”

Section: Ezetimibe a Novel Potent And Specific Cholesterol Absorptmentioning

confidence: 99%

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Cholesterol metabolism and therapeutic targets: Rationale for targeting multiple metabolic pathways

Turley

2004

Clin Cardiol

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The liver is the major regulator of the plasma low density lipoprotein cholesterol (LDL‐C) concentration because it is not only the site of formation of very low density lipoproteins (VLDL), the precursors of most LDL in the circulation, but it is also the organ where the bulk of receptor‐mediated clearance of LDL takes place. The liver also initially clears all the cholesterol that is absorbed from the small intestine. The absorption of excess cholesterol can potentially increase the amount of cholesterol stored in the liver. This, in turn, can result in increased VLDL secretion, and hence LDL formation, and also downregulation of hepatic LDL receptor activity. Such events will potentially increase plasma LDL‐C levels. The converse situation occurs when cholesterol absorption is inhibited. Cholesterol enters the lumen of the small intestine principally from bile and diet. The major steps involved in the absorption process have been characterized. On average, about half of all cholesterol entering the intestine is absorbed, but the fractional absorption rate varies greatly among individuals. While the basis for this variability is not understood, it may partly explain why some patients respond poorly or not at all to statins and other classes of lipid‐lowering drugs. There are few data relating to racial differences in cholesterol absorption. One study reported a significantly higher rate in African Americans compared with non‐African Americans. Multiple lipid‐lowering drugs that target pathways involving the absorption, synthesis, transport, storage, catabolism, and excretion of cholesterol are available. Ezetimibe selectively blocks cholesterol absorption and lowers plasma LDL‐C levels by an average of 18%. When ezetimibe is coadministered with lower doses of statins, there is an additive reduction in LDL‐C level, which equals the reduction achieved with maximal doses of statins alone. Dual inhibition of cholesterol synthesis and absorption is an effective new strategy for treating hypercholesterolemia.

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Section: Efficacy Of Combination Therapy Using Ezetimibe With a Statinmentioning

confidence: 79%

Section: Ezetimibe a Novel Potent And Specific Cholesterol Absorptmentioning

confidence: 99%

Cholesterol metabolism and therapeutic targets: Rationale for targeting multiple metabolic pathways

Turley

2004

Clin Cardiol

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“…Ezetimibe can be coadministered with any statin and will provide a mean LDL-C reduction of 18% to 25%. In a study by Gagne et al (29), only 19% of selected patients reached treatment goals on statin monotherapy and the addition of ezetimibe brought this figure to 72%.…”

Section: Effect On Cholesterol Tg and Lipoprotein Lipidsmentioning

confidence: 98%

Combination of statin and ezetimibe for the treatment of dyslipidemias and the prevention of coronary artery disease

Genest

2006

Canadian Journal of Cardiology

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“…In the management of hypertension, it is reasonable for physicians to combine many drugs with different modes of action to achieve the recommended lipid concentration (2). Some studies have investigated a new cholesterol absorption inhibitor (ezetimibe) in combination with statins (3)(4)(5)(6). Ezetimibe is the first member in a class of selective cholesterol absorption inhibitors that works by impairing the intestinal reabsorption of hepatically excreted biliary cholesterol and dietary cholesterol (7,8).…”

mentioning

confidence: 99%

“…Recently, Fux et al (13) described two cases of myopathy associated with a statinezetimibe association. In previous papers evaluating this specific association (3)(4)(5)(6), the investigators did not provide sufficient information about adverse muscular events. In these studies, only patients receiving statins in combination with ezetimibe complained of muscle pain and/or had creatine kinase (CK) elevations 10 or more times the upper limit of normal (3)(4)(5)(6).…”

mentioning

confidence: 99%

Ezetimibe-associated myopathy in monotherapy and in combination with a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor

Simard

Poirier

2006

Canadian Journal of Cardiology

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Efficacy and safety of ezetimibe added to ongoing statin therapy for treatment of patients with primary hypercholesterolemia

Cited by 459 publications

References 13 publications

Cholesterol metabolism and therapeutic targets: Rationale for targeting multiple metabolic pathways

Cholesterol metabolism and therapeutic targets: Rationale for targeting multiple metabolic pathways

Combination of statin and ezetimibe for the treatment of dyslipidemias and the prevention of coronary artery disease

Ezetimibe-associated myopathy in monotherapy and in combination with a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor

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