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Rosuvastatin/Ezetimibe: A Review in Hypercholesterolemia

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Abstract

Rosuvastatin/ezetimibe combines two lipid-lowering agents: rosuvastatin, an HMG-CoA reductase inhibitor (i.e. statin) with particularly strong inhibitory effects on hepatic cholesterol synthesis, and ezetimibe, which inhibits the intestinal absorption of cholesterol. A fixed-dose combination (FDC) of rosuvastatin/ezetimibe is indicated as an adjunctive therapy to diet for the management of primary hypercholesterolemia in adults in numerous countries worldwide. In well-designed clinical trials evaluating the therapeutic efficacy of rosuvastatin/ezetimibe administered as either separate agents or as an FDC, rosuvastatin/ezetimibe was significantly more effective than rosuvastatin monotherapy (including at double the dose of rosuvastatin) or simvastatin/ezetimibe in reducing low-density lipoprotein cholesterol (LDL-C) and total cholesterol in adults with hypercholesterolemia. Furthermore, rosuvastatin/ezetimibe enabled significantly higher proportions of patients to achieve recommended LDL-C levels than rosuvastatin monotherapy or simvastatin/ezetimibe. Rosuvastatin/ezetimibe did not significantly differ from rosuvastatin monotherapy with respect to incidences of treatment-related or serious adverse events in these short-term trials and displayed a similar safety profile to simvastatin/ezetimibe. While additional cardiovascular outcomes data and head-to-head comparisons with atorvastatin/ezetimibe would be of interest, rosuvastatin/ezetimibe is a potent and generally well-tolerated drug combination that extends the range of options available for the pharmacological management of primary hypercholesterolemia in adults.

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Acknowledgements

During the peer review process, the manufacturer of rosuvastatin/ezetimibe was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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    Yvette N. Lamb

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The preparation of this review was not supported by any external funding.

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Yvette Lamb is a salaried employee of Adis International Ltd/Springer Nature, is responsible for the article content and declares no relevant conflicts of interest.

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Enhanced material for this Adis Drug Evaluation can be found at https://doi.org/10.6084/m9.figshare.12408062.

The manuscript was reviewed by:K. Awad, Faculty of Medicine, Zagazig University, Zagazig, Egypt; L. Ose, Department of Nutrition, University of Oslo, Oslo, Norway; A. A. S. M. Soares, Faculty of Medicine, University of Brasilia, Brasilia, Brazil.

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Lamb, Y.N. Rosuvastatin/Ezetimibe: A Review in Hypercholesterolemia. Am J Cardiovasc Drugs 20, 381–392 (2020). https://doi.org/10.1007/s40256-020-00421-1

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