PCSK9 Inhibitors: A New Era of Lipid Lowering Therapy.
Publication/Presentation Date
2-2017
Abstract
Hyperlipidemia is a well-established risk factor for developing cardiovascular disease (CVD). The recent American College of Cardiology and American Heart Association guidelines on lipid management emphasize treatment of individuals at increased risk for developing CVD events with 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors (statins) at doses proven to reduce CVD events. However, there are limited options for patients who are either intolerant to statin therapy, develop CVD despite being on maximally tolerated statin therapy, or have severe hypercholesterolemia. Recently the Food and Drug Administration approved two novel medications for low-density lipoprotein (LDL)-cholesterol reduction: Evolocumab and Alirocumab. These agents target and inactivate proprotein convertase subtilsin-kexin type 9 (PCSK9), a hepatic protease that attaches and internalizes LDL receptors into lysosomes hence promoting their destruction. By preventing LDL receptor destruction, LDL-C levels can be lowered 50%-60% above that achieved by statin therapy alone. This review explores PCSK-9 biology and the mechanisms available to alter it; clinical trials targeting PCSK9 activity, and the current state of clinically available inhibitors of PCSK9.
Volume
9
Issue
2
First Page
76
Last Page
91
ISSN
1949-8462 (online)
Published In/Presented At
Chaudhary R, Garg J, Shah N, Sumner A.(2017). PCSK9 inhibitors: A new era of lipid lowering therapy. World J Cardiol 2017; 9(2): 76-91
Disciplines
Cardiology | Medical Sciences | Medicine and Health Sciences
PubMedID
28289523
Department(s)
Department of Medicine, Cardiology Division
Document Type
Article