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Related Experiment Video

Updated: Aug 25, 2025

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PCSK9 Inhibition: From Current Advances to Evolving Future.

Chunping Liu1,2,3, Jing Chen4, Huiqi Chen1

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|October 14, 2022
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Summary

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors lower LDL-C by targeting LDL-R. This review details PCSK9 inhibitor applications, mechanisms, and progress in cardiovascular and other diseases.

Keywords:
PCSK9 inhibitorscardiovascular diseaseclinical applicationsresearch statussecurity

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Cardiovascular Medicine

Background:

  • Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a liver-secreted serine protease.
  • PCSK9 primarily degrades the low-density lipoprotein receptor (LDL-R), reducing LDL-C clearance.

Purpose of the Study:

  • To systematically review the application, preclinical studies, safety, mechanism of action, and research progress of PCSK9 inhibitors.
  • To provide insights for drug development and clinical application of PCSK9 inhibitors in cardiovascular diseases.
  • To explore the expansion of PCSK9 inhibitor applications in other diseases.

Main Methods:

  • Literature review of existing studies on PCSK9 inhibitors.
  • Systematic summary of preclinical and clinical data.
  • Analysis of the mechanisms of action and safety profiles.

Main Results:

  • PCSK9 inhibitors target LDL-R, reducing LDL-C levels.
  • PCSK9 inhibitors also interact with other receptors like TLRs, CD36, LRP1, ApoER2, and VLDL-R, impacting lipoprotein concentration and thrombosis.
  • Marketed inhibitors include alirocumab, evolocumab, and inclisiran; others like small molecules, nucleic acid drugs, and vaccines are in development.

Conclusions:

  • PCSK9 inhibitors are effective in managing cardiovascular diseases by lowering LDL-C.
  • PCSK9 has potential therapeutic applications beyond cardiovascular diseases, including pancreatic cancer, sepsis, and Parkinson's disease.
  • Further research and development are needed to optimize PCSK9 inhibitor therapies and expand their clinical utility.