Ezetimibe: A Selective Cholesterol Absorption Inhibitor

Edith A. Nutescu, Pharm.D.; Nancy L. Shapiro, Pharm.D.


Pharmacotherapy. 2003;23(11) 

In This Article


Ezetimibe has been studied in monotherapy, in combination therapy with statins, in combination therapy with fenofibrate, and in difficult-to-treat populations, such as those with HeFH, HoFH, and sitosterolemia. Clinical data demonstrate consistent benefits of ezetimibe in reducing LDL, triglyceride, and total cholesterol levels, and in increasing HDL levels. Ezetimibe is not metabolized through the CYP enzyme system, and no clinically significant drug interactions have been reported. Side effects have been similar to those of placebo when administered as monotherapy and in combination with statins.

Ezetimibe is an effective and safe new option for treating hyperlipidemia and may be most beneficial in combination therapy, allowing for administration of lower statin doses. Future studies are warranted to assess the effect of ezetimibe on cardiovascular morbidity and mortality.


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