Cholesterol-lowering drugs: Focus on Ezetimibe

Cholesterol-lowering drugs: Focus on ezetimibe

Harold E. Bays
Louisville Metabolic and Atherosclerosis Research Center, Louisville, KY, USA


Ezetimibe is an intestinal cholesterol/sterol inhibitor. It is generally well-tolerated, and except for coadministration with cyclosporin (which increases concentration of both ezetimibe and cyclosporin), has limited drug interactions. Clinical trial data suggests that ezetimibe 10 mg orally once a day reduces low density lipoprotein cholesterol (LDL-C) levels about 15-25% as monotherapy or when added to statins, depending on the patient and individual clinical trial. Ezetimibe also reduces lipoprotein remnants. Due to its additive effects to statins, international lipid guidelines recommend ezetimibe as an option for patients who do not achieve LDL-C treatment goals with statins alone. The Improved Reduction of Outcomes: Vytorin Efficacy International Trial (IMPROVE-IT) trial demonstrated that when added to statin therapy, ezetimibe incrementally lowered LDL-C levels and modestly improved cardiovascular outcomes. Ezetimibe is formulated as monotherapy, or as a fixed-dose combination with statins or bempedoic acid. Finally, ezetimibe is the only pharmacotherapy approved for treatment of beta-sitosterolemia, which is a rare autsomal recessive disorder resulting in enhanced intestinal cholesterol absorption, increased circulating sterols, and tendinous and cutaneous xanthomas, arthritis or arthralgia, and premature cardiovascular disease.


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