Alirocumab for the treatment of hypercholesterolemia

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

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Introduction: Alirocumab is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) that is administered by subcutaneous injection every 2 weeks. Area covered: Herein, the authors discuss the background to inhibition of PCSK9 and the pharmacodynamics, pharmacokinetics and clinical trials with alirocumab. Alirocumab produces substantial reductions in low density lipoprotein cholesterol (LDL-C) in patients with and without background statin treatment. The safety profile appears very promising from the relatively short term studies that have been completed but there are some remaining concerns about long term risks of neurocognitive events and developing diabetes. Expert opinion: The profound reduction in LDL-C with alirocumab is most likely to translate into cardiovascular benefits in the ODYSSEY OUTCOMES trial and is unlikely in itself to result in any major adverse effects. The high cost and the current lack of long-term safety and efficacy data will restrict the use of alirocumab to patients who have high cardiovascular risk from established atherosclerotic cardiovascular disease or heterozygous familial hypercholesterolemia and who are unable to achieve LDL-C targets with maximally tolerated dose of statins with or without other lipid-lowering drugs. When further data become available, these indications are likely to be expanded.

Original languageEnglish
Pages (from-to)1-11
Number of pages11
JournalExpert Opinion on Biological Therapy
DOIs
Publication statusAccepted/In press - Mar 20 2017

Fingerprint

Hypercholesterolemia
Proprotein Convertases
LDL Cholesterol
Hydroxymethylglutaryl-CoA Reductase Inhibitors
Subtilisin
Pharmacodynamics
Therapeutics
Safety
Hyperlipoproteinemia Type II
Pharmacokinetics
Maximum Tolerated Dose
Expert Testimony
Subcutaneous Injections
Medical problems
Cardiovascular Diseases
Monoclonal Antibodies
alirocumab
Clinical Trials
Lipids
Costs and Cost Analysis

Keywords

  • Alirocumab
  • atherosclerotic cardiovascular disease
  • heterozygous familial hypercholesterolemia
  • low-density lipoprotein cholesterol
  • proprotein convertase subtilisin/kexin type 9

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Clinical Biochemistry

Cite this

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

In: Expert Opinion on Biological Therapy, 20.03.2017, p. 1-11.

Research output: Contribution to journalArticle

Tomlinson, Brian ; Hu, Miao ; Zhang, Yuzhen ; Chan, Paul ; Liu, Zhong Min. / Alirocumab for the treatment of hypercholesterolemia. In: Expert Opinion on Biological Therapy. 2017 ; pp. 1-11.
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