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American Journal of Cardiovascular Drugs

20.12.2024 | Review Article

Inclisiran as a siRNA Inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9); Past, Present, and Future

verfasst von: Taha Mansoor, Bassam Hamid Rao, Kartik Gupta, Sachin S. Parikh, Dmitry Abramov, Anurag Mehta, Mahmoud Al Rifai, Salim S. Virani, Vijay Nambi, Abdul Mannan Khan Minhas, Santhosh K. G. Koshy

Erschienen in: American Journal of Cardiovascular Drugs

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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.

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Titel: Inclisiran as a siRNA Inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9); Past, Present, and Future
verfasst von: Taha Mansoor
Bassam Hamid Rao
Kartik Gupta
Sachin S. Parikh
Dmitry Abramov
Anurag Mehta
Mahmoud Al Rifai
Salim S. Virani
Vijay Nambi
Abdul Mannan Khan Minhas
Santhosh K. G. Koshy
Publikationsdatum: 20.12.2024
Verlag: Springer International Publishing
Erschienen in: American Journal of Cardiovascular Drugs
Print ISSN: 1175-3277
Elektronische ISSN: 1179-187X
DOI: https://doi.org/10.1007/s40256-024-00712-x

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