Related Experiment Video

Updated: Feb 15, 2026

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
08:14

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9

Published on: August 28, 2018

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The evolving therapeutic landscape of PCSK9 inhibition

Brett S Mansfield1, Yakubu Bene-Alhasan2, Christie M Ballantyne3

  • 1Carbohydrate & Lipid Metabolism Research Unit, Department of Internal Medicine, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, South Africa.

Atherosclerosis
|February 13, 2026
PubMed

Insights

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors lower LDL cholesterol, reducing cardiovascular disease risk. Approved therapies and novel treatments offer new options for managing hypercholesterolemia.

Area of Science:

  • Cardiovascular Medicine
  • Genetics
  • Pharmacology

Background:

  • Cardiovascular disease is a leading global cause of death.
  • Low-density lipoprotein (LDL) cholesterol is a major modifiable risk factor.
  • Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates LDL receptor expression, influencing LDL cholesterol levels.

Purpose of the Study:

  • To review the evidence for approved PCSK9 inhibitors.
  • To discuss novel PCSK9-targeted therapies in development.
  • To explore expanding indications for PCSK9 inhibition.

Main Methods:

  • Review of scientific literature on PCSK9 inhibitors.
  • Summary of clinical trial data for approved therapies.
  • Discussion of emerging therapeutic strategies, including gene editing.

Main Results:

  • Loss-of-function PCSK9 variants confirm its role as a therapeutic target.
  • PCSK9 inhibitors (monoclonal antibodies, siRNA, oral agents) effectively lower LDL-C.
  • Genetic validation supports PCSK9 as a target for hypercholesterolemia.

Conclusions:

  • PCSK9 inhibition is a validated strategy for managing hypercholesterolemia.
  • A range of PCSK9-targeted therapies are available and in development.
  • PCSK9 inhibition shows promise for broader cardiovascular disease prevention.

Keywords:
Atherosclerotic cardiovascular diseaseCardiovascular riskLDL cholesterolLipid-lowering therapyPCSK9

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