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Reviews in Cardiovascular Medicine  2018, Vol. 19 Issue (S1): 31-46     DOI: 10.3909/ricm19S1S0002
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PCSK9 Inhibitors: Mechanism of Action, Efficacy, and Safety
Eli M. Roth1, Michael H. Davidson2
1 Sterling Research Group, Cincinnati, OH
2 Department of Cardiology, University of Chicago Medicine, Chicago, IL
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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.
Key words:  PCSK9      Low-density lipoprotein receptors      Monoclonal antibodies      Familial hypercholesterolemia     
Published:  20 January 2018     

Cite this article: 

Eli M. Roth, Michael H. Davidson. PCSK9 Inhibitors: Mechanism of Action, Efficacy, and Safety. Reviews in Cardiovascular Medicine, 2018, 19(S1): 31-46.

URL: 

https://rcm.imrpress.com/EN/10.3909/ricm19S1S0002     OR     https://rcm.imrpress.com/EN/Y2018/V19/IS1/31

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