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Evolocumab: A Review in Hyperlipidemia

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Abstract

Evolocumab (Repatha®) is a monoclonal antibody targeting proprotein convertase subtilisin/kexin type 9 (PCSK9) that is administered subcutaneously at a dosage of 140 mg every 2 weeks or 420 mg once monthly. Across 12-week phase III trials in patients with primary hypercholesterolemia or mixed dyslipidemia, evolocumab was more effective than placebo (treatment difference −54.8 to −76.3 %) and/or ezetimibe (treatment difference −36.9 to −47.2 %) at reducing low-density lipoprotein cholesterol (LDL-C) levels, including when added to statin therapy, when administered to statin-intolerant patients, when administered as monotherapy, and in patients with heterozygous familial hypercholesterolemia who were receiving statins with or without other lipid-lowering drugs. Evolocumab also significantly lowered LDL-C levels (treatment difference of ≈30 % vs. placebo) in patients with homozygous familial hypercholesterolemia when added to statins with or without ezetimibe in a 12-week phase III trial. The efficacy of evolocumab was maintained in the longer term, and it was well tolerated. In conclusion, subcutaneous evolocumab is a valuable new treatment for use in primary hypercholesterolemia or mixed dyslipidemia and homozygous familial hypercholesterolemia, particularly in patients unable to reach LDL-C goals despite treatment with statins with or without other lipid-lowering therapies and in patients who do not tolerate or are not able to receive statins.

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Acknowledgments

During the peer review process, the manufacturer of evolocumab 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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    Gillian M. Keating

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Correspondence to Gillian M. Keating.

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

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Gillian Keating is a salaried employee of Adis/Springer, is responsible for the article content and declares no relevant conflicts of interest.

Additional information

The manuscript was reviewed by: A. Hirayama, Division of Cardiology, Department of Medicine, Nihon University School of Medicine, Tokyo, Japan; G. K. Hovingh, Department of Vascular Medicine, Academic Medical Center, Amsterdam, the Netherlands; J. Mansourati, Department of Cardiology, University Hospital of Brest, Hôpital de la Cavale Blanche, Brest, France; A. G. Olsson, Department of Medical and Health Sciences, Linköping University, Linköping, Sweden; K. G. Parhofer, Medizinische Klinik II—Grosshadern, Klinikum der Universität München, Munich, Germany; G. F. Watts, School of Medicine and Pharmacology, University of Western Australia, Western Australia, Australia.

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Keating, G.M. Evolocumab: A Review in Hyperlipidemia. Am J Cardiovasc Drugs 16, 67–78 (2016). https://doi.org/10.1007/s40256-015-0153-0

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