Rosuvastatin and ezetimibe for the treatment of dyslipidemia and hypercholesterolemia

ABSTRACT

Introduction: Statins are powerful lipid-lowering agents which reduce cardiovascular (CV)–related morbidity and mortality. However, a large proportion of patients cannot attain the target low-density lipoprotein cholesterol (LDL-C) levels, despite receiving maximally tolerated doses of high-intensity statins. Also, adherence to treatment may be reduced due to statin-induced myopathy or other side effects. For these reasons, guidelines recommend adding the cholesterol absorption inhibitor ezetimibe.

Areas covered: Authors discuss the main pharmacological characteristics of rosuvastatin and ezetimibe, their lipid-lowering and pleiotropic effects, as well as the clinical effects of the fixed dose combination of these drugs when used to treat dyslipidemia.

Expert opinion: The rosuvastatin/ezetimibe combination is safe and effective in patients with hypercholesterolemia or dyslipidemia with or without diabetes and with or without cardiovascular disease. This drug combination enabled higher proportions of patients to achieve recommended LDL-C goals than rosuvastatin monotherapy or the simvastatin/ezetimibe combination, without additional adverse events. Despite the lack of additional CV outcomes data and comparisons with atorvastatin/ezetimibe, rosuvastatin/ezetimibe appears as a potent and generally well-tolerated drug combination eligible for the management of hypercholesterolemia and dyslipidemia in adults. Recently, the 40 mg rosuvastatin/10 mg ezetimibe fixed combination was approved and is also evaluated.

KEYWORDS:

• Hypercholesterolemia
• rosuvastatin
• ezetimibe
• combination
• fixed combination
• safety
• effectiveness

Article highlights

• Rosuvastatin lowers plasma LDL-C levels by inhibiting HMG-CoA reductase activity.

• Ezetimibe lowers plasma LDL-C levels by inhibiting the absorption of cholesterol from the small intestine.

• The combination of the 2 drugs act in an additive way.

• The fixed combination of the two drugs is more effective than each drug administered as monotherapy.

• The fixed dose combination (FDC) of the 2 drugs is safe and cost-effective.

• Studies are needed to verify the expected reduction in cardiovascular events with this FDC.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosure

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.