Which medications in the drug class PCSK9 Inhibitors are used in the treatment of Coronary Artery Atherosclerosis?

Updated: Apr 09, 2021
  • Author: Sandy N Shah, DO, MBA, FACC, FACP, FACOI; Chief Editor: Yasmine S Ali, MD, MSCI, FACC, FACP  more...
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Answer

PCSK9 Inhibitors

Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors decrease LDLR degradation by PCSK9, and thereby improve LDL-C clearance and lower plasma LDL-C. On July 24, 2015, the FDA gave approval for the first PCSK9 inhibitor, alirocumab. [119]

Alirocumab (Praluent)

Alirocumab is a monoclonal antibody that binds to PCSK9. LDL-C is cleared from the circulation preferentially through the LDL receptor (LDLR) pathway. PCSK9 is a serine protease that destroys LDLR in the liver, resulting in decreased LDL-C clearance and increased plasma LDL-C. PCSK9 inhibitors decrease LDLR degradation by PCSK9.

Alirocumab is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia (HeFH) or clinical atherosclerotic cardiovascular disease, who require additional lowering of LDL-C. It was also approved by the FDA as adjunctive therapy for homozygous familial hypercholesterolemia. 

Additionally, alirocumab is indicated for the prevention of cardiovascular (CV) events, as it has been shown to reduce risk of MI, stroke, and unstable angina requiring hospitalization in adults with established cardiovascular disease. 

Evolocumab (Repatha)

Evolocumab is a monoclonal antibody that inhibits the serine protease PCSK9. PCSK9 destroys the LDL receptor in the liver, thereby decreasing LDL-C clearance. This agent is indicated as an adjunct to diet and maximally tolerated statin therapy for the treatment of adults with heterozygous familial hypercholesterolemia (HeFH) or clinical atherosclerotic CVD, who require additional lowering of LDL-C.

Evolocumab is also indicated as an adjunct to diet and other LDL-lowering therapies (eg, statins, ezetimibe, LDL apheresis) for the treatment of adults and adolescents aged 13-17 y with homozygous familial hypercholesterolemia (HoFH) who require additional lowering of LDL-C.


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