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Description: Ezetimibe is an anti-hyperlipidemic medication which is used to lower cholesterol levels. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes.
Drug Type: Small Molecule; Approved
Pharmacology: Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe, administered alone is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia. It is also used in combination therapy with HMG-CoA reductase inhibitors. Ezetimibe has a mechanism of action that differs from those of other classes of cholesterol-reducing compounds (HMG-CoA reductase inhibitors, bile acid sequestrants, fibric acid derivatives, and plant stanols). Ezetimibe does not inhibit cholesterol synthesis in the liver, or increase bile acid excretion but instead localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of HMG-CoA reductase inhibitors.
Mechanism of Action: Ezetimibe localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver.
Indication: For use as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia.
Half Life: 22 hours
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Data Correlations | 8 studies

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Genes category icon Genes
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NPC1L1 100 100
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Individual Studies

  • Simvastatin treatment of HPBM-macrophages

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    HMG-CoA reductase inhibitors, statins, have beneficial vascular effects beyond their cholesterol-lowering action. These pleiotropic effects include an anti-inflammatory effect on macrophages. Since macrophages play a central role in atherogenesis, we further characterized the effects on peripheral b…

    Authors: Tuomisto T Tiina, Lumivuori Henri, Kansanen Emilia et al.

    Organization: A.I.Virtanen Institute Molecular Medicin…

  • Mouse lung samples treated with Simvastatin with or without LPS induced inflammation

    Mus musculus Mus musculus | RNA Expression   RNA Expression

    Study explored the effect of simvastatin in a murine inflammatory model of ALI and finds significant protection is afforded by simvastatin on LPS-induced lung vascular leak and inflammation implicating a potential role for statins in managing ALI.

    Authors: Jacobson J, Barnard J, Ma S et al.

    Organization: Johns Hopkins University 5501 Hopkins Ba…
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Associated Researchers

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Thought leaders and organizations working on research involving ezetimibe.

View All Author iconAuthors
  • Dieter Lütjohann
  • Thomas Sudhop
  • Klaus von Bergmann
  • Diane L Tribble
  • Barry Gumbiner
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Merck
  • Schering-Plough
  • National Heart, Lung, and Blood Institute (NHLBI)
  • University of California, San Diego
  • Children's Hospital & Research Center Oakland
View All Affiliations icon Organizations
  • Liver Center and Gastroenterology Division
  • University Medical Center Utrecht
  • Osaka University Graduate School of Medicine
  • University of Western Ontario
  • University of Bonn

Clinical Trials | 214 trials

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