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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Radcliffe Medical Media
2021
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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) |
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DOAJ |
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Diseases of the circulatory (Cardiovascular) system RC666-701 |
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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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1718372720247308288 |