Ezetimibe; More Than a Low Density Lipoprotein Cholesterol Lowering Drug? An Update After 4 Years

Eirini      Lioudaki; Emmanuel      S. Ganotakis; Dimitri      P. Mikhailidis

Abstract

Ezetimibe (EZE), a selective inhibitor of intestinal cholesterol absorption, is mostly used in combination with statins across various patient populations. Besides its low-density lipoprotein cholesterol (LDL-C) lowering, EZE exerts different effects on several other variables. In an earlier review, we discussed the effects of EZE on lipid parameters other than LDL-C [e.g. C-reactive protein (CRP) levels, insulin sensitivity and endothelial function]. In the present review, we consider recent evidence regarding these topics as well as data reporting novel EZE actions. EZE may protect from cholelithiasis and non-alcoholic fatty liver disease (NAFLD) and appears as an effective lipid-lowering treatment option for human-immunodeficiency virus (HIV)-positive patients, transplant recipients and children with familial hypercholesterolaemia (FH). Studies with EZE that raised concern about its effects on atherosclerosis are also discussed. The potential clinical benefit of these actions with respect to vascular events and overall mortality remains to be established in appropriately designed trials.

Keywords: Ezetimibe, pleiotropic, C-reactive protein, insulin sensitivity, endothelial function, statin, intestinal cholesterol absorption, low-density lipoprotein cholesterol, C-reactive protein (CRP) levels, chole-lithiasis, non-alcoholic fatty liver disease, lipid-lowering treatment, human-immunodeficiency virus, familial hypercholestero-laemia (FH), atherosclerosis, Niemann-Pick, enterocyte brush border membrane, phytos-terol, fat soluble vitamins, blood pressure, triglycerides, apolipo-protein, glucose, insulin resistance, metabolic syndrome, endothelial dysfunction, cholelithiasis, transplant, liver, adverse, creatine kinase, renal function, non-alcoholic, platelet, randomized controlled trials, coronary artery dis-ease [E-R(CAD)], diabetes mel-litus (DM), metabolic syndrome (MetS), Simvastatin, ENHANCE, cIMT, hsCRP, CASHMERE, atorvastatin, Atherosclerosis Progression, SANDS, VYCTOR, confidence interval, apolipoprotein (apo), triglycerides (TG), chylomicron, EZE Plus Simvastatin, Fenofibrate, Niacin, Resins, Orlistat/Rimonabant