Ezetimibe (CAS: 163222-33-1)
Background Information of Ezetimibe
Ezetimibe, a cholesterol-absorption inhibitor, reduces levels of low-density lipoprotein (LDL) cholesterol when added to statin treatment.
Storage Condition of Ezetimibe
Quality Control and Spectral Data
Mechanism and Indications
Structure Information of Ezetimibe
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Other Form Products of Ezetimibe
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Chemical and Physical Properties
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.Xiaobo Lin, Susan B. Racette, Michael Lefevre, et al. Combined Effects of Ezetimibe and Phytosterols on Cholesterol Metabolism: A Randomized, Controlled Feeding Study in Humans. Circulation. 2011; 124(5): 596-601.
Both ezetimibe and phytosterols inhibit cholesterol absorption. We tested the hypothesis that ezetimibe combined with phytosterols is more effective than ezetimibe alone in altering cholesterol metabolism.
Methods and Results
Twenty-one mildly hypercholesterolemic subjects completed a randomized, double-blind, placebo-controlled, triple crossover study. Each subject received a phytosterol-controlled diet plus (1) ezetimibe placebo + phytosterol placebo, (2) 10 mg ezetimibe/day + phytosterol placebo, and (3) 10 mg ezetimibe/day + 2.5 g phytosterols/day, for 3 weeks each. All meals were prepared in a metabolic kitchen. Primary outcomes were intestinal cholesterol absorption, fecal cholesterol excretion, and LDL cholesterol levels. The combined treatment resulted in significantly lower intestinal cholesterol absorption (598 mg/day, 95% CI 368 to 828) relative to control (2161 mg/day, 1112 to 3209) and ezetimibe alone (1054 mg/day, 546 to 1561, both P < 0.0001). Fecal cholesterol excretion was significantly greater (P < 0.0001) with combined treatment (962 mg/day, 757 to 1168) relative to control (505 mg/day, 386 to 625) and ezetimibe alone (794 mg/day, 615 to 973). Plasma LDL cholesterol values during control, ezetimibe alone, and ezetimibe + phytosterols averaged 129 (95% CI: 116 to 142), 108 (97 to 119), and 101 (90 to 112) mg/dL (P < 0.0001 relative to control).
The addition of phytosterols to ezetimibe significantly enhanced the effects of ezetimibe on whole-body cholesterol metabolism and plasma LDL cholesterol. The large cumulative action of combined dietary and pharmacologic treatment on cholesterol metabolism emphasizes the potential importance of dietary phytosterols as adjunctive therapy for the treatment of hypercholesterolemia.
.Anne B. Rosseb?, Terje R. Pedersen, Kurt Boman, et al. Intensive Lipid Lowering with Simvastatin and Ezetimibe in Aortic Stenosis. N Engl J Med 2008; 359:1343-1356.
.John J.P. Kastelein, Fatima Akdim, Erik S.G. Stroes, et al. Simvastatin with or without Ezetimibe in Familial Hypercholesterolemia. N Engl J Med ,2008; 358:1431-1443.
.Christie M. Ballantyne, John Houri, Alberto Notarbartolo, et al. Effect of Ezetimibe Coadministered With Atorvastatin in 628 Patients With Primary Hypercholesterolemia. Clinical Investigation and Reports Circulation. 2003; 107: 2409-2415.
.Claude Gagne?, Harold E. Bays, Stuart R. Weiss, et al. Efficacy and Safety of Ezetimibe Added to Ongoing Statin Therapy for Treatment of Patients With Primary Hypercholesterolemia. Am J Cardiol 2002;90:1084-1091.