Introduction: Although
statin therapy is a powerful
lipid-lowering strategy, only one-fifth of
statin users currently reach their
lipid goals. In addition,
statin treatment alone has relatively low efficacy in reducing other
lipid fractions than
low-density lipoprotein-cholesterol (
LDL-C). In such cases, most guidelines recommend adding the
cholesterol absorption inhibitor
ezetimibe.Areas covered: This paper summarizes the main pharmacological characteristics of
rosuvastatin and
ezetimibe (mechanism of action, metabolism), their
lipid-lowering and pleiotropic effects, with particular attention to the clinical effects of the combined drugs in
hypercholesterolemia and mixed
dyslipidemia patients (such as the ones affected by
diabetes mellitus and
Acquired Immune Deficiency Syndrome (
AIDS)).Expert opinion: The additive effect of
rosuvastatin and
ezetimibe helps to reach
lipid goals in a large number of high-risk patients, while avoiding some safety issues related to high dosages of intensive
statin therapy. Patients with diabetes receive additional benefits from
ezetimibe as they seem to absorb
cholesterol more effectively than non-diabetic ones, because of increased NPC1L1 gene expression.
Ezetimibe augments
rosuvastatin triglyceride-lowering and anti-inflammatory effects, as well. Taking into account its excellent safety profile and lack of clinically relevant
drug-drug interactions, the
rosuvastatin/
ezetimibe association is a valuable alternative to
statin dose uptitration.