Ezetimibe reduces low-density lipoprotein cholesterol: results of a phase III, randomized, double-blind, placebo-controlled trial

Knopp, Robert H.; Gitter, H.; Truitt, Tyler; Lipka, Leslie J.; LeBeaut, Alexandre; Suresh, Ramachandran; Veltri, Enrico P.

doi:10.1016/s1567-5688(01)80027-1

Cited by 31 publications

(26 citation statements)

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“…Ezetimibe localizes at the epithelial brush border of the small intestine and inhibits the absorption of cholesterol and phytosterols without affecting the absorption of TGs and fatsoluble vitamins (16,17,19). The likely molecular target for ezetimibe is the Niemann-Pick C1 Like 1 (NPC1L1), a membrane-associated protein.…”

Section: Pharmacological and Pharmacokinetic Propertiesmentioning

confidence: 99%

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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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Section: Pharmacological and Pharmacokinetic Propertiesmentioning

confidence: 99%

“…Two studies (19,28) with a sufficient number of subjects evaluated the efficacy and safety of ezetimibe (10 mg) monotherapy in patients with mild to moderate hypercholesterolemia. Dujovne et al (28) and Knopp et al (19) enrolled 892 and 827 patients, respectively.…”

Section: Effect On Cholesterol Tg and Lipoprotein Lipidsmentioning

confidence: 99%

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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“…Ezetimibe is a potent and selective inhibitor of cholesterol absorption that has been shown to reduce the overall delivery of cholesterol to the liver, thereby promoting the synthesis of LDL receptors, with a subsequent reduction of serum LDL-C. 6,7 In addition to inhibiting cholesterol absorption, ezetimibe also inhibits net phytosterol absorption. Its mechanism of action is different from that of other intestinalacting lipid-altering agents such as phytosterols/phytostanols, resins, and polymers.…”

Section: What Is the Mechanism Of Action Of Ezetimibe?mentioning

confidence: 99%

Perspectives in Cholesterol-Lowering Therapy

2003

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“…The clinical efficacy of ezetimibe in humans has recently been demonstrated both in monotherapy [83,89,91,92] as well as in combined therapy with other lipid-lowering drugs [93][94][95][96][97][98][99].…”

Section: Selective Cholesterol Absorption Inhibitor: Ezetimibementioning

confidence: 99%

New drugs for the treatment of hypercholesterolaemia

Iglesias¹,

Díez

2003

Expert Opinion on Investigational Drugs

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Endogenous and exogenous pathways determine plasma levels of cholesterol and lipoproteins. Plasma cholesterol levels and coronary heart disease risk can be reduced pharmacologically by decreasing cholesterol synthesis, increasing its elimination and/or reducing its absorption from the intestine. The more profound knowledge about cholesterol homeostasis has allowed the development of several lipid-lowering drugs with different mechanisms of action, with the purpose of reducing both morbidity and mortality associated with coronary heart disease. Two new and more potent 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins), also called superstatins (rosuvastatin and pitavastatin), are being studied for their ability to improve lipid profiles. Rosuvastatin is a potent, hepato-selective and relatively hydrophilic statin with a low propensity for muscle toxicity and drug interactions. Pitavastatin is another statin with a high oral bioavailability and minimal propensity for cytochrome p450-mediated drug interactions. Rosuvastatin seems to be more potent than other available statins while pitavastatin presents with a similar potency to that of atorvastatin. Another promising approach for lowering total and low-density lipoprotein cholesterol levels is inhibition of cholesterol absorption. A wide variety of new agents with the capacity for inhibiting the intestinal cholesterol absorption is currently being investigated. Ezetimibe is a selective cholesterol absorption inhibitor whose clinical efficacy has been recently demonstrated both in monotherapy and in combination with other lipid-lowering drugs. Colesevelam, a new bile acid sequestrant, has shown a clinical efficacy similar to that of other resins, with minimal gastrointestinal side effects, improving tolerability and patient compliance. Other lipid-lowering drugs with the ability to act at the enterocyte level, such as avasimibe and implitapide, are currently being investigated in humans.

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Ezetimibe reduces low-density lipoprotein cholesterol: results of a phase III, randomized, double-blind, placebo-controlled trial

Cited by 31 publications

References 0 publications

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

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

Perspectives in Cholesterol-Lowering Therapy

New drugs for the treatment of hypercholesterolaemia

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