Inclisiran as a siRNA inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9); past, present, and future
Document Type
Article
Department
Medicine; Cardiology; Office of the Provost
Abstract
Reducing low-density lipoprotein cholesterol (LDL-C) levels has been shown to reduce the risk of developing atherosclerotic cardiovascular disease (ASCVD). Statins are the foundation of LDL-C lowering therapy with other non-statin agents used in circumstances where goal LDL-C levels are not reached or owing to intolerance to adverse effects of statins. In 2003, the discovery of the role of the proprotein convertase subtilisin/kexin type 9 (PCSK9) system in promoting elevated LDL-C levels led to new avenues of drug development to achieve target LDL-C. In 2021, inclisiran, a small interfering ribonucleic acid (siRNA) molecule targeting PCSK9 was approved by the Food and Drug Administration (FDA). Inclisiran has demonstrated effective reductions of LDL-C, such as in the large phase-3 ORION-9, ORION-10, and ORION-11 trials in which it achieved LDL-C reductions of 39.7%, 52.3%, and 49.9%, respectively. This review discusses the current clinical evidence and ongoing clinical studies of inclisiran as well as analyzes other areas of PCSK9 inhibition development.
Publication (Name of Journal)
American Journal of Cardiovascular Drugs
DOI
10.1007/s40256-024-00712-x
Recommended Citation
Mansoor, T.,
Rao, B. H.,
Gupta, K.,
Parikh, S. S.,
Abramov, D.,
Mehta, A.,
Rifai, M. A.,
Virani, S. S.,
Nambi, V.,
Minhas, A. K.,
Koshy, S. K.
(2024). Inclisiran as a siRNA inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9); past, present, and future. American Journal of Cardiovascular Drugs.
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Comments
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