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Drugs for hypercholesterolaemia - from statins to pro-protein convertase subtilisin kexin 9 (PCSK9) inhibition

Anthony S Wierzbicki1, Paul Grant2

  • 1Guy's and St Thomas' Hospitals, London, UK Anthony.wierzbicki@kcl.ac.uk.

Clinical Medicine (London, England)
|August 3, 2016
PubMed

Insights

New therapies targeting pro-protein convertase subtilisin kexin 9 (PCSK9) offer a novel approach to lowering low-density lipoprotein cholesterol (LDL-C) and reducing cardiovascular disease (CVD) risk. These PCSK9 inhibitors are poised to change hypercholesterolemia management.

Area of Science:

  • Cardiovascular medicine
  • Lipidology
  • Pharmacology

Background:

  • Cardiovascular disease (CVD) is a leading cause of global mortality.
  • Elevated low-density lipoprotein cholesterol (LDL-C) significantly increases CVD risk.
  • Statins and ezetimibe are current hypercholesterolemia treatments.

Purpose of the Study:

  • To review the role of pro-protein convertase subtilisin kexin 9 (PCSK9) in lipid metabolism.
  • To discuss novel PCSK9 inhibitor therapeutics.
  • To explore the clinical application of PCSK9 inhibitors pending outcome studies.

Main Methods:

  • Review of existing literature on PCSK9 function and its genetic variants.
  • Analysis of data on newly developed PCSK9-targeted therapies (alirocumab, evolocumab).
  • Discussion of potential clinical integration of PCSK9 inhibitors.

Main Results:

  • PCSK9 regulates LDL receptor expression, influencing LDL-C levels.
  • Inactivating PCSK9 mutations are associated with reduced LDL-C and CVD events.
  • Monoclonal antibodies targeting PCSK9 have been developed and licensed.

Conclusions:

  • PCSK9 inhibition represents a promising therapeutic strategy for hypercholesterolemia.
  • Alirocumab and evolocumab offer new options for managing high LDL-C.
  • Clinical utility will be further defined by ongoing large-scale CVD outcome trials.

Keywords:
Cardiovascular diseasePSCK9 inhibitorshyperlipidaemiastatins

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