195
Views
9
CrossRef citations to date
0
Altmetric
Preliminary Communication

Rapid effects of different lipid-lowering drugs on PCSK9 in humans

, , &
Pages 519-524 | Published online: 18 Jan 2017

References

  • Cariou B, Le May C, Costet P. Clinical aspects of PCSK9. Atherosclerosis 216, 258–265 (2011). ▪ Excellent review of PCSK9 and its clinical significance.
  • Lagace TA, Curtis DE, Garuti R et al. Secreted PCSK9 decreases the number of LDL receptors in hepatocytes and in livers of parabiotic mice. J. Clin. Invest. 116, 2995–3005 (2006).
  • Careskey HE, Davis RA, Alborn WE, Troutt JS, Cao G, Konrad RJ. Atorvastatin increases human serum levels of proprotein convertase subtilisin/kexin type 9. J. Lipid. Res. 49, 394–398 (2008). ▪▪ The first study investigating the effects of statins on PCSK9 in humans.
  • Welder G, Zineh I, Pacanowski MA, Troutt JS, Cao G, Konrad RJ. High-dose atorvastatin causes a rapid sustained increase in human serum PCSK9 and disrupts its correlation with LDL cholesterol. J. Lipid. Res. 51, 2714–2721 (2010).
  • Awan Z, Seidah NG, MacFadyen JG et al. Rosuvastatin, proprotein convertase subtilisin/kexin type 9 concentrations, and LDL cholesterol response: the JUPITER Trial. Clin. Chem. 58, 183–189 (2012).
  • Troutt JS, Alborn WE, Cao G, Konrad RJ. Fenofibrate treatment increases human serum proprotein convertase subtilisin kexin type 9 levels. J. Lipid. Res. 51, 345–351 (2010).
  • Pandor A, Ara RM, Tumur I et al. Ezetimibe monotherapy for cholesterol lowering in 2,722 people: systematic review and meta-analysis of randomized controlled trials. J. Intern. Med. 265, 568–580 (2009).
  • Morrone D, Weintraub WS, Toth PP et al. Lipid-altering efficacy of ezetimibe plus statin and statin monotherapy and identification of factors associated with treatment response: a pooled analysis of over 21,000 subjects from 27 clinical trials. Atherosclerosis 223, 251–261 (2012).
  • Lu Z, Kou W, Du B et al. Effect of Xuezhikang, an extract from red yeast chinese rice, on coronary events in a chinese population with previous myocardial infarction. Am. J. Cardiol. 101, 1689–1693 (2008).
  • Becker DJ, Gordon RY, Halbert SC, French B, Morris PB, Rader DJ. Red yeast rice for dyslipidemia in statin-intolerant patients: a randomized trial. Ann. Intern. Med. 150, 830–839 (2009).
  • Expert Panel on Detection, Evaluation, Treatment of High Blood Cholesterol in Adults. Executive summary of the third report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, 14 Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III). JAMA 285, 2486–2497 (2001).
  • Davignon J, Dubuc G. Statins and ezetimibe modulate plasma proprotein convertase subtilisin kexin-9 (PCSK9) levels. Trans. Am. Clin. Climatol. Assoc. 120, 163–173 (2009).
  • Bays HE, Neff D, Tomassini JE, Tershakovec AM. Ezetimibe: cholesterol lowering and beyond. Expert Rev. Cardiovasc. Ther. 6, 447–470 (2008).
  • Dubuc G, Chamberland A, Wassef H et al. Statins upregulate PCSK9, the gene encoding the proprotein convertase neural apoptosisregulated convertase-1 implicated in familial hypercholesterolemia. Arterioscl. Thromb. Vasc. Biol. 24, 1454–1459 (2004). ▪▪ The first preclinical study reporting that statins upregulate PCSK9.
  • Dubuc G, Tremblay M, Paré G et al. A new method for measurement of total plasma PCSK9: clinical applications. J. Lipid Res. 51, 140–149 (2010).
  • Koren MJ, Scott R, Kim JB et al. Efficacy, safety, and tolerability of a monoclonal antibody to proprotein convertase subtilisin/ kexin type 9 as monotherapy in patients with hypercholesterolaemia (MENDEL): a randomised, double-blind, placebocontrolled, Phase 2 study. Lancet 380, 1995–2006 (2012).
  • Lakoski SG, Lagace TA, Cohen JC, Horton JD, Hobbs HH. Genetics and metabolic determinants of plasma PCSK9 levels. J. Clin. Endocrinol. Metab. 94, 2537–2543 (2009).
  • Berthold HK, Seidah NG, Benjannet S, Gouni-Berthold I. Evidence from a randomized trial that simvastatin, but not ezetimibe, upregulates circulating PCSK9 levels. PLoS ONE 8, e60095 (2013).
  • Costet P, Hoffmann MM, Cariou B, Guyomarc’h Delasalle B, Konrad T, Winkler K. Plasma PCSK9 is increased by fenofibrate and atorvastatin in a non-additive fashion in diabetic patients. Atherosclerosis 212, 246–251 (2010).
  • Michelena HI, Osorio LA, Citkowitz E. Cholesterol levels after 3 days of high-dose simvastatin in patients at moderate to high risk for coronary events. Int. J. Cardiol. 101, 111–114 (2005).
  • Persson L, Cao G, Ståhle L et al. Circulating proprotein convertase subtilisin kexin type 9 has a diurnal rhythm synchronous with cholesterol synthesis and is reduced by fasting in humans.Arterioscler. Thromb. Vasc. Biol. 30, 2666–2672 (2010).
  • Stein EA, Gipe D, Bergeron J et al. Effect of a monoclonal antibody to PCSK9, REGN727/SAR236553, to reduce low-density lipoprotein cholesterol in patients with heterozygous familial hypercholesterolaemia on stable statin dose with or without ezetimibe therapy: a Phase 2 randomised controlled trial. Lancet 380, 29–36 (2012).
  • McKenney JM, Koren MJ, Kereiakes DJ, Hanotin C, Ferrand A-C, Stein EA. Safety and efficacy of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 serine protease, SAR236553/REGN727, in patients with primary hypercholesterolemia receiving ongoing stable atorvastatin therapy. J. Am. Coll. Cardiol. 59, 2344–2353 (2012).

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.