Evolocumab for the treatment of hypercholesterolemia

Brian Tomlinson, Miao Hu, Yuzhen Zhang, Paul Chan, Zhong Min Liu

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Introduction: Evolocumab is a fully human monoclonal immunoglobulin G2 directed against human proprotein convertase subtilisin/kexin type 9 (PCSK9). It is administered by subcutaneous injection every 2 weeks or once monthly. Area covered: Herein, the authors discuss the rationale for inhibiting PCSK9 and describe the pharmacodynamics, pharmacokinetics and clinical trials with evolocumab. Evolocumab reduces low density lipoprotein cholesterol (LDL-C) levels by 50 to 60% in most patients with and without background treatment with statins or other lipid lowering agents. The safety profile appears satisfactory from the completed clinical studies and concerns regarding the risk of neurocognitive events have largely been dispelled. Expert opinion: The reduction of LDL-C with evolocumab to previously unattainable levels has resulted in a reduction in the composite cardiovascular event endpoint in the FOURIER trial and this is likely to impact on future lipid management guidelines. The clinical outcome data and excellent tolerability profile clearly support the use of evolocumab in patients at high cardiovascular risk, including those with heterozygous or homozygous familial hypercholesterolemia, who are unable to achieve LDL-C targets with statins with or without other lipid-lowering drugs. The high cost of evolocumab will restrict its use, however.

Original languageEnglish
Pages (from-to)1-15
Number of pages15
JournalExpert Opinion on Biological Therapy
DOIs
Publication statusAccepted/In press - Aug 13 2017

Fingerprint

Hypercholesterolemia
LDL Cholesterol
Hydroxymethylglutaryl-CoA Reductase Inhibitors
Lipids
Therapeutics
Pharmacodynamics
Proprotein Convertases
Subtilisin
Hyperlipoproteinemia Type II
Pharmacokinetics
Expert Testimony
Subcutaneous Injections
AMG 145
Immunoglobulins
Clinical Trials
Guidelines
Safety
Costs and Cost Analysis
Composite materials
Pharmaceutical Preparations

Keywords

  • Atherosclerotic cardiovascular disease
  • evolocumab
  • heterozygous familial hypercholesterolemia
  • homozygous familial hypercholesterolemia
  • low-density lipoprotein cholesterol
  • proprotein convertase subtilisin/kexin type 9

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry

Cite this

Evolocumab for the treatment of hypercholesterolemia. / Tomlinson, Brian; Hu, Miao; Zhang, Yuzhen; Chan, Paul; Liu, Zhong Min.

In: Expert Opinion on Biological Therapy, 13.08.2017, p. 1-15.

Research output: Contribution to journalArticle

Tomlinson, Brian ; Hu, Miao ; Zhang, Yuzhen ; Chan, Paul ; Liu, Zhong Min. / Evolocumab for the treatment of hypercholesterolemia. In: Expert Opinion on Biological Therapy. 2017 ; pp. 1-15.
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