Current Evidence and Future Directions of PCSK9 Inhibition

Recent scientific and therapeutic advances in proprotein convertase subtilisin kexin type 9 (PCSK9) inhibition have opened a chapter in the management of hypercholesterolemia, especially in patients who are inadequately controlled on or intolerant to statins. The two PCSK9 monoclonal antibodies, evo...

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Autores principales: Jiaqian Xu, Michael D Shapiro
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Lenguaje:EN
Publicado: Radcliffe Medical Media 2021
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Acceso en línea:https://doaj.org/article/1545b531fe6049699ec45ed8e3e0f060
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spelling oai:doaj.org-article:1545b531fe6049699ec45ed8e3e0f0602021-12-04T16:03:54ZCurrent Evidence and Future Directions of PCSK9 Inhibition10.15420/usc.2020.171758-390X1758-3896https://doaj.org/article/1545b531fe6049699ec45ed8e3e0f0602021-02-01T00:00:00Zhttps://www.uscjournal.com/articleindex/usc.2020.17https://doaj.org/toc/1758-3896https://doaj.org/toc/1758-390XRecent scientific and therapeutic advances in proprotein convertase subtilisin kexin type 9 (PCSK9) inhibition have opened a chapter in the management of hypercholesterolemia, especially in patients who are inadequately controlled on or intolerant to statins. The two PCSK9 monoclonal antibodies, evolocumab and alirocumab, reduce LDL cholesterol by 60% and improve cardiovascular outcomes when taken in addition to statin therapy. More recently, inclisiran, a silencing RNA (siRNA) that inhibits translation of PCSK9 mRNA, demonstrated LDL cholesterol reduction by 45–50% with the advantage of dramatically reduced dose frequency. Other modes of PCSK9 inhibition include small molecule antagonists, vaccines, CRISPR gene editing, and antagonism at various steps of translation, and post-translational processing.Jiaqian XuMichael D ShapiroRadcliffe Medical MediaarticleDiseases of the circulatory (Cardiovascular) systemRC666-701ENUS Cardiology Review , Vol 15, Iss , Pp - (2021)
institution DOAJ
collection DOAJ
language EN
topic Diseases of the circulatory (Cardiovascular) system
RC666-701
spellingShingle Diseases of the circulatory (Cardiovascular) system
RC666-701
Jiaqian Xu
Michael D Shapiro
Current Evidence and Future Directions of PCSK9 Inhibition
description Recent scientific and therapeutic advances in proprotein convertase subtilisin kexin type 9 (PCSK9) inhibition have opened a chapter in the management of hypercholesterolemia, especially in patients who are inadequately controlled on or intolerant to statins. The two PCSK9 monoclonal antibodies, evolocumab and alirocumab, reduce LDL cholesterol by 60% and improve cardiovascular outcomes when taken in addition to statin therapy. More recently, inclisiran, a silencing RNA (siRNA) that inhibits translation of PCSK9 mRNA, demonstrated LDL cholesterol reduction by 45–50% with the advantage of dramatically reduced dose frequency. Other modes of PCSK9 inhibition include small molecule antagonists, vaccines, CRISPR gene editing, and antagonism at various steps of translation, and post-translational processing.
format article
author Jiaqian Xu
Michael D Shapiro
author_facet Jiaqian Xu
Michael D Shapiro
author_sort Jiaqian Xu
title Current Evidence and Future Directions of PCSK9 Inhibition
title_short Current Evidence and Future Directions of PCSK9 Inhibition
title_full Current Evidence and Future Directions of PCSK9 Inhibition
title_fullStr Current Evidence and Future Directions of PCSK9 Inhibition
title_full_unstemmed Current Evidence and Future Directions of PCSK9 Inhibition
title_sort current evidence and future directions of pcsk9 inhibition
publisher Radcliffe Medical Media
publishDate 2021
url https://doaj.org/article/1545b531fe6049699ec45ed8e3e0f060
work_keys_str_mv AT jiaqianxu currentevidenceandfuturedirectionsofpcsk9inhibition
AT michaeldshapiro currentevidenceandfuturedirectionsofpcsk9inhibition
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