Ezetimibe: rationale and role in the management of hypercholesterolemia

Clinical Cardiology
Leonid YatskarArthur Schwartzbard

Abstract

Elevated low-density lipoprotein (LDL) cholesterol plays an important role in the development of atherosclerosis. In part, plasma LDL levels are dependent on cholesterol absorption in the intestine and the rate of intrinsic cholesterol synthesis. Therapy with 3-hydroxy-3-methylglutaryl coenzyme A-reductase inhibitors has often proven to be successful in reducing plasma LDL levels. However, a significant number of patients do not reach their target LDL levels despite statin therapy. As is reviewed, drugs that inhibit cholesterol absorption are a useful adjunct to lipid-lowering therapy by statins. This review discusses the mechanisms involved in intestinal absorption of cholesterol and its transport as potential targets of newer agents that affect cholesterol absorption. The use of bile acid sequestrants and esters of plant stanols, as well as other intestinally active agents for reducing plasma LDL levels, has been limited by side effects and difficulties in patient compliance. In contrast, the new selective cholesterol transporter inhibitor ezetimibe has been demonstrated to reduce plasma LDL alone or in combination with statins without significant adverse effects. In spite of the robust lipid-lowering data with ezetimibe, que...Continue Reading

References

Oct 1, 1987·European Journal of Clinical Investigation·Y A Kesäniemi, T A Miettinen
Nov 16, 1995·The New England Journal of Medicine·T A MiettinenE Vartiainen
Nov 26, 1999·The Journal of Nutrition·T T Nguyen
Nov 22, 2000·Current Opinion in Lipidology·J PlatR P Mensink
Jun 30, 2001·The New England Journal of Medicine·P M RidkerUNKNOWN Air Force/Texas Coronary Atherosclerosis Prevention Study Investigators
Aug 21, 2002·Circulation·Richard C PasternakUNKNOWN National Heart, Lung and Blood Institute
Oct 9, 2002·Circulation·Thomas SudhopKlaus von Bergmann
Nov 9, 2002·The American Journal of Cardiology·Claude GagnéUNKNOWN Ezetimibe Study Group
Nov 9, 2002·The American Journal of Cardiology·Carlos A DujovneUNKNOWN Ezetimibe Study Group
Dec 31, 2002·Journal of the American College of Cardiology·Michael H DavidsonEnrico P Veltri
Feb 21, 2004·Science·Scott W AltmannMichael P Graziano
Jun 15, 2004·The American Journal of Cardiology·Christie M BallantyneJoanne Palmisano
Mar 10, 2005·The New England Journal of Medicine·John C LaRosaUNKNOWN Treating to New Targets (TNT) Investigators
Nov 17, 2005·JAMA : the Journal of the American Medical Association·Terje R PedersenUNKNOWN Incremental Decrease in End Points Through Aggressive Lipid Lowering (IDEAL) Study Group

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Citations

Jun 1, 2006·Expert Review of Neurotherapeutics·Walter J Lukiw
Jun 10, 2008·Expert Opinion on Emerging Drugs·Walter J Lukiw
Jan 18, 2015·Indian Heart Journal·K Sarat ChandraSeema Gulati
Jul 29, 2006·Pharmacology & Therapeutics·Irina A Pikuleva

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