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Related Experiment Video

Updated: Sep 26, 2025

A High-Throughput Luciferase Assay to Evaluate Proteolysis of the Single-Turnover Protease PCSK9
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[Update on PCSK9 inhibition].

Julius L Katzmann1, Florian Custodis2, Stephan H Schirmer3,4

  • 1Klinik und Poliklinik für Kardiologie, Universitätsklinikum Leipzig, Liebigstraße 20, 04103, Leipzig, Deutschland. julius.katzmann@medizin.uni-leipzig.de.

Herz
|April 21, 2022
PubMed
Summary

Newer subcutaneous PCSK9 inhibitors, including antibodies and RNA interference therapies like inclisiran, effectively lower LDL cholesterol for cardiovascular prevention. These treatments offer improved efficacy and convenience, with inclisiran requiring only biannual administration.

Keywords:
AlirocumabCoronary artery diseaseEvolocumabInclisiranLDL cholesterol

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Related Experiment Videos

Last Updated: Sep 26, 2025

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Area of Science:

  • Cardiovascular Medicine
  • Pharmacology
  • Biotechnology

Background:

  • Lowering low-density lipoprotein (LDL) cholesterol is crucial for cardiovascular disease prevention.
  • Subcutaneous proprotein convertase subtilisin-kexin type 9 (PCSK9) inhibitors are established lipid-lowering therapies.
  • Current options include monoclonal antibodies (evolocumab, alirocumab) and RNA interference (inclisiran).

Purpose of the Study:

  • To review the role and advancements in PCSK9 inhibition for lipid management.
  • To highlight the efficacy and administration profiles of novel PCSK9 inhibitors.
  • To discuss ongoing research and future strategies in PCSK9 inhibition.

Main Methods:

  • Review of existing literature on PCSK9 inhibitors.
  • Analysis of clinical trial outcomes for subcutaneous PCSK9 antibodies.
  • Description of the mechanism of action for inclisiran via RNA interference.

Main Results:

  • Subcutaneous PCSK9 antibodies (evolocumab, alirocumab) reduce LDL cholesterol by ~60% with good tolerability.
  • Inclisiran, an RNA interference agent, inhibits PCSK9 synthesis intracellularly and requires administration every 6 months.
  • Both antibody therapies have demonstrated reduction in cardiovascular endpoints in major trials.

Conclusions:

  • PCSK9 inhibitors represent a significant advancement in cardiovascular prevention.
  • Inclisiran offers a novel, less frequent dosing regimen for PCSK9 inhibition.
  • Ongoing research explores oral PCSK9 inhibitors and gene editing for future cardiovascular risk reduction.