Reviews in Cardiovascular Medicine (RCM) is published by IMR Press from Volume 19 Issue 1 (2018). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) license, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement with MedReviews, LLC.
PCSK9 Inhibitors: Mechanism of Action, Efficacy, and Safety
Eli M. Roth 1, Michael H. Davidson 2
Affiliations
Article Info
1 Sterling Research Group, Cincinnati, OH
2 Department of Cardiology, University of Chicago Medicine, Chicago, IL
Abstract
Low-density lipoprotein (LDL) receptors on the surface of liver hepatocytes are the primary way that humans regulate serum LDL cholesterol levels. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a proteolytic enzyme that indirectly regulates serum LDL cholesterol (LDL-C) by causing the destruction of LDL receptors. Less LDL receptors result in increased LDL-C in the bloodstream but inhibiting or binding the circulating PCSK9 results in increased LDL receptors with the resultant decrease in serum LDL-C. Two PCSK9 inhibitors are currently approved for use: alirocumab and evolocumab. Both are fully human monoclonal antibodies that bind free PCSK9. Herein we discuss the mechanism of action, efficacy, and safety of PCSK9 inhibitors.
Keywords
- PCSK9
- Low-density lipoprotein receptors
- Monoclonal antibodies
- Familial hypercholesterolemia