Current Evidence and Future Directions of PCSK9 Inhibition

Recent scientific and therapeutic advances in proprotein convertase subtilisin kexin type 9 (PCSK9) inhibition have opened a chapter in the management of hypercholesterolemia, especially in patients who are inadequately controlled on or intolerant to statins. The two PCSK9 monoclonal antibodies, evo...

Full description

Saved in:
Bibliographic Details
Main Authors: Jiaqian Xu, Michael D Shapiro
Format: Article
Language:English
Published: Radcliffe Medical Media 2021-02-01
Series:US Cardiology Review
Online Access:https://www.uscjournal.com/articleindex/usc.2020.17
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Recent scientific and therapeutic advances in proprotein convertase subtilisin kexin type 9 (PCSK9) inhibition have opened a chapter in the management of hypercholesterolemia, especially in patients who are inadequately controlled on or intolerant to statins. The two PCSK9 monoclonal antibodies, evolocumab and alirocumab, reduce LDL cholesterol by 60% and improve cardiovascular outcomes when taken in addition to statin therapy. More recently, inclisiran, a silencing RNA (siRNA) that inhibits translation of PCSK9 mRNA, demonstrated LDL cholesterol reduction by 45–50% with the advantage of dramatically reduced dose frequency. Other modes of PCSK9 inhibition include small molecule antagonists, vaccines, CRISPR gene editing, and antagonism at various steps of translation, and post-translational processing.
ISSN:1758-3896
1758-390X