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Diseases 2018, 6(3), 63; https://doi.org/10.3390/diseases6030063

Inclisiran: A New Promising Agent in the Management of Hypercholesterolemia

1
Department of Medicine, Division of Cardiology, Mount Sinai Hospital, New York, NY 11357, USA
2
Department of Medicine, Mount Sinai St. Luke’s-West Hospital, New York, NY 10025, USA
3
School of Medicine, University of Crete, 71003 Heraklion, Greece
4
Cardiology Clinic, Cardiology Unlimited, PC, New York, NY 10033, USA
5
Department of Medicine, Division of Cardiology, Montefiore Medical Center, Bronx, NY 10467, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Ahmed Bakillah
Received: 29 June 2018 / Revised: 11 July 2018 / Accepted: 11 July 2018 / Published: 13 July 2018
Full-Text   |   PDF [566 KB, uploaded 13 July 2018]   |  

Abstract

The discovery of proprotein convertase subtilisin-kexin type 9 (PCSK9), a serine protease which binds to the low-density lipoprotein (LDL) receptors and targets the receptors for lysosomal degradation, offered an additional route through which plasma LDL-cholesterol (LDL-C) levels can be controlled. Initially, the therapeutic approaches to reduce circulating levels of PCSK9 were focused on the use of monoclonal antibodies. To that effect, evolocumab and alirocumab, two human monoclonal antibodies directed against PCSK9, given on a background of statin therapy, have been shown to markedly decrease LDL-C levels and significantly reduce cardiovascular risk. The small interfering RNA (siRNA) molecules have been used recently to target the hepatic production of PCSK9. siRNA interferes with the expression of specific genes with complementary nucleotide sequences by affecting the degradation of mRNA post-transcription, thus preventing translation. Inclisiran is a long-acting, synthetic siRNA directed against PCSK9 and it has been shown to significantly decrease hepatic production of PCSK9 and cause a marked reduction in LDL-C levels. This review aims to present and discuss the current clinical and scientific evidence pertaining to inclisiran, which is a new promising agent in the management of hypercholesterolemia. View Full-Text
Keywords: proprotein convertase subtilisin-kexin type 9 (PCSK9); small interfering RNA (siRNA); inclisiran; low-density lipoprotein-cholesterol (LDL-C); cardiovascular disease (CVD); cardiovascular risk proprotein convertase subtilisin-kexin type 9 (PCSK9); small interfering RNA (siRNA); inclisiran; low-density lipoprotein-cholesterol (LDL-C); cardiovascular disease (CVD); cardiovascular risk
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Kosmas, C.E.; Muñoz Estrella, A.; Sourlas, A.; Silverio, D.; Hilario, E.; Montan, P.D.; Guzman, E. Inclisiran: A New Promising Agent in the Management of Hypercholesterolemia. Diseases 2018, 6, 63.

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