Literature DB >> 35445838

[Update on PCSK9 inhibition].

Julius L Katzmann1, Florian Custodis2, Stephan H Schirmer3,4, Ulrich Laufs5.   

Abstract

Lowering of low-density lipoprotein (LDL) cholesterol represents one of the most effective interventions in cardiovascular prevention. Besides the oral treatment with statins, ezetimibe and bempedoic acid, subcutaneously administered inhibitors of proprotein convertase subtilisin-kexin type 9 (PCSK9) have been established as further cornerstones of lipid-lowering treatment. The antibodies evolocumab and alirocumab are administered subcutaneously every 2-4 weeks and lower LDL cholesterol by around 60%, independent of pre-treatment with very good tolerability. Both drugs successfully reduced cardiovascular endpoints in large outcome trials. A novel principle of PCSK9 inhibition is RNA interference, which is exploited by the novel compound inclisiran. Inclisiran is a double-stranded modified RNA molecule, which neutralizes the mRNA of PCSK9 and thus inhibits PCSK9 protein synthesis intracellularly. Inclisiran only needs to be administered every 6 months. The cardiovascular outcome trial ORION‑4 is currently ongoing. In Germany, prescription of PCSK9 inhibitors is regulated by the decision of the Federal Joint Committee. Novel strategies to inhibit PCSK9 function are under development and include orally available drugs and animal experiment concepts on gene editing, which are in different states of evaluation.
© 2022. The Author(s), under exclusive licence to Springer Medizin Verlag GmbH, ein Teil von Springer Nature.

Entities:  

Keywords:  Alirocumab; Coronary artery disease; Evolocumab; Inclisiran; LDL cholesterol

Mesh:

Substances:

Year:  2022        PMID: 35445838     DOI: 10.1007/s00059-022-05112-y

Source DB:  PubMed          Journal:  Herz        ISSN: 0340-9937            Impact factor:   1.443


  34 in total

1.  Sequence variations in PCSK9, low LDL, and protection against coronary heart disease.

Authors:  Jonathan C Cohen; Eric Boerwinkle; Thomas H Mosley; Helen H Hobbs
Journal:  N Engl J Med       Date:  2006-03-23       Impact factor: 91.245

Review 2.  PCSK9 inhibitors: clinical evidence and implementation.

Authors:  Marc S Sabatine
Journal:  Nat Rev Cardiol       Date:  2019-03       Impact factor: 32.419

3.  Lipid-Reduction Variability and Antidrug-Antibody Formation with Bococizumab.

Authors:  Paul M Ridker; Jean-Claude Tardif; Pierre Amarenco; William Duggan; Robert J Glynn; J Wouter Jukema; John J P Kastelein; Albert M Kim; Wolfgang Koenig; Steven Nissen; James Revkin; Lynda M Rose; Raul D Santos; Pamela F Schwartz; Charles L Shear; Carla Yunis
Journal:  N Engl J Med       Date:  2017-03-17       Impact factor: 91.245

4.  Secreted PCSK9 decreases the number of LDL receptors in hepatocytes and in livers of parabiotic mice.

Authors:  Thomas A Lagace; David E Curtis; Rita Garuti; Markey C McNutt; Sahng Wook Park; Heidi B Prather; Norma N Anderson; Y K Ho; Robert E Hammer; Jay D Horton
Journal:  J Clin Invest       Date:  2006-11       Impact factor: 14.808

5.  Mutations in PCSK9 cause autosomal dominant hypercholesterolemia.

Authors:  Marianne Abifadel; Mathilde Varret; Jean-Pierre Rabès; Delphine Allard; Khadija Ouguerram; Martine Devillers; Corinne Cruaud; Suzanne Benjannet; Louise Wickham; Danièle Erlich; Aurélie Derré; Ludovic Villéger; Michel Farnier; Isabel Beucler; Eric Bruckert; Jean Chambaz; Bernard Chanu; Jean-Michel Lecerf; Gerald Luc; Philippe Moulin; Jean Weissenbach; Annick Prat; Michel Krempf; Claudine Junien; Nabil G Seidah; Catherine Boileau
Journal:  Nat Genet       Date:  2003-06       Impact factor: 38.330

6.  The secretory proprotein convertase neural apoptosis-regulated convertase 1 (NARC-1): liver regeneration and neuronal differentiation.

Authors:  Nabil G Seidah; Suzanne Benjannet; Louise Wickham; Jadwiga Marcinkiewicz; Stephanie Belanger Jasmin; Stefano Stifani; Ajoy Basak; Annik Prat; Michel Chretien
Journal:  Proc Natl Acad Sci U S A       Date:  2003-01-27       Impact factor: 11.205

Review 7.  Low-density lipoproteins cause atherosclerotic cardiovascular disease. 1. Evidence from genetic, epidemiologic, and clinical studies. A consensus statement from the European Atherosclerosis Society Consensus Panel.

Authors:  Brian A Ference; Henry N Ginsberg; Ian Graham; Kausik K Ray; Chris J Packard; Eric Bruckert; Robert A Hegele; Ronald M Krauss; Frederick J Raal; Heribert Schunkert; Gerald F Watts; Jan Borén; Sergio Fazio; Jay D Horton; Luis Masana; Stephen J Nicholls; Børge G Nordestgaard; Bart van de Sluis; Marja-Riitta Taskinen; Lale Tokgözoglu; Ulf Landmesser; Ulrich Laufs; Olov Wiklund; Jane K Stock; M John Chapman; Alberico L Catapano
Journal:  Eur Heart J       Date:  2017-08-21       Impact factor: 29.983

8.  Association of medication adherence and depression with the control of low-density lipoprotein cholesterol and blood pressure in patients at high cardiovascular risk.

Authors:  Julius L Katzmann; Felix Mahfoud; Michael Böhm; Martin Schulz; Ulrich Laufs
Journal:  Patient Prefer Adherence       Date:  2018-12-18       Impact factor: 2.711

9.  Variation in PCSK9 and HMGCR and Risk of Cardiovascular Disease and Diabetes.

Authors:  Brian A Ference; Jennifer G Robinson; Robert D Brook; Alberico L Catapano; M John Chapman; David R Neff; Szilard Voros; Robert P Giugliano; George Davey Smith; Sergio Fazio; Marc S Sabatine
Journal:  N Engl J Med       Date:  2016-12-01       Impact factor: 91.245

Review 10.  Physiological and therapeutic regulation of PCSK9 activity in cardiovascular disease.

Authors:  Simon Glerup; Rainer Schulz; Ulrich Laufs; Klaus-Dieter Schlüter
Journal:  Basic Res Cardiol       Date:  2017-04-24       Impact factor: 17.165

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