Evolocumab: Considerations for the Management of Hyperlipidemia
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Purpose of Review
To review the efficacy, safety, pharmacology, and pharmacokinetics of evolocumab, a proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor.
PCSK9 inhibitors are a class of lipid-lowering agents that significantly reduce low-density lipoprotein cholesterol (LDL-C) levels in patients with atherosclerotic cardiovascular disease and hyperlipidemia. Evolocumab is a monoclonal antibody that inhibits PCSK9 and has been evaluated in phase II and III studies as monotherapy, in combination with statins and other lipid-lowering therapies, in patients who are statin intolerant, and in patients with heterozygous and homozygous familial hypercholesterolemia. Data from these studies show that evolocumab significantly reduces LDL-C levels. Treatment with evolocumab also significantly improves levels of other lipid parameters (e.g., apolipoproteins A1 and B, lipoprotein(a), non–high-density lipoprotein cholesterol, and triglycerides). Recent results indicate that LDL-C reduction with evolocumab significantly reduces the risk of cardiovascular events and is also associated with atherosclerotic plaque regression. From a safety standpoint, rates of adverse events (AEs), serious AEs, and AEs leading to discontinuation were similar between evolocumab and controls in clinical trials, and no increase in AEs was observed when evolocumab was used in combination with statins.
Patients with elevated LDL-C benefit from evolocumab treatment, suggesting that evolocumab could help meet an unmet medical need in high-risk patient populations with atherosclerotic cardiovascular disease and hyperlipidemia that are unable to reduce LDL-C levels sufficiently with statin therapy alone.
KeywordsLow-density lipoprotein cholesterol PCSK9 Statins Evolocumab
The authors acknowledge Meghan Johnson, PhD, of Complete Healthcare Communications, LLC, whose work was funded by Amgen, and Annalise M. Nawrocki, PhD, of Amgen Inc., for writing and editorial assistance.
Compliance with Ethical Standards
Conflict of Interest
Barbara S. Wiggins has served as a consultant for Amgen Inc. Helina Kassahun, Armando Lira, and Ransi Somaratne are employees of Amgen Inc. and hold Amgen stock and/or stock options. Ransi Somaratne is an inventor on at least one pending patent application owned by Amgen Inc. relating to evolocumab. Jeffrey Senfield declares no conflict of interest.
Human and Animal Rights and Informed Consent
This article does not contain any studies with human or animal subjects performed by any of the authors.
Papers of particular interest, published recently, have been highlighted as: • Of importance •• Of major importance
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