Ezetimibe, an inhibitor of intestinal
cholesterol absorption, can decrease total
cholesterol (TC),
low density lipoprotein cholesterol (
LDL-C),
triglycerides (TGs) and
apolipoprotein (
apo) B levels and increase
high-density lipoprotein cholesterol (HDL-C) levels. Apart from
lipid-lowering,
ezetimibe may exert certain off-target actions (e.g. anti-inflammatory, anti-atherogenic and
antioxidant) thus contributing to a further decrease of
cardiovascular disease (CVD) risk.Ezetimibe trials resulted in controversial outcomes with some studies reporting
atherosclerosis regression and reductions in CVD events following
ezetimibe therapy in combination with a
statin while others reported negative results. The results of the ongoing IMProved Reduction of Outcomes:
Vytorin Efficacy International Trial (IMPROVE-IT) which compares
ezetimibe plus
simvastatin with
simvastatin monotherapy with regard to CVD outcomes after
acute coronary syndromes should further elucidate the effect of
ezetimibe on CVD events.This review presents the results of up-to-date clinical trials with
ezetimibe and summarizes its potential pleiotropic effects. Furthermore, we comment on the administration of
ezetimibe in treating high-risk patients [i.e. with
diabetes mellitus (DM),
metabolic syndrome (MetS),
non-alcoholic fatty liver disease (
NAFLD),
chronic kidney disease (CKD),
peripheral artery disease (PAD) or carotid disease]. The use of
ezetimibe either as monotherapy or as add-on
therapy in daily clinical practice is also discussed.