Efficacy and safety profile of evolocumab (AMG145), an injectable inhibitor of the proprotein convertase subtilisin/kexin type 9: the available clinical evidence

Bibliography

• Maxwell KN, Breslow JL. Adenoviral mediated expression of PCSK9 in mice results in a low-density lipoprotein receptor knockout phenotype. Proc Natl Acad Sci USA 2004;101:7100-5
   PubMed Web of Science ®Google Scholar
• Abifadel M, Varret M, Rabee JD, et al. Mutations in PCSK9 cause autosomal dominant hypercholesterolemia. Nat Genet 2003;34:154-6
   PubMed Web of Science ®Google Scholar
• Cohen JC, Boerwinkle E, Mosley TH Jr, Hobbs HH. Sequence variations in PCSK9, low LDL, and protection against coronary heart disease. N Engl J Med 2006;354:1264-7
   PubMed Web of Science ®Google Scholar
• Urban D, Pöss J, Böhm M, Laufs U. Targeting the proprotein convertase subtisilin/kexin type 9 for the treatment of dyslipidemia and atherosclerosis. J Am Coll Cardiol 2013;62:1401-8
   PubMed Web of Science ®Google Scholar
• Rashid S, Curtis DE, Garuti R, et al. Decreased plasma cholesterol and hypersensitivity to statins in mice lacking Pcsk9. Proc Natl Acad Sci USA 2005;102:5374-9
   PubMed Web of Science ®Google Scholar
• Farnier M. PCSK9 inhibitors. Curr Opin Lipidol 2013;24:251-8
   PubMed Web of Science ®Google Scholar
• Stein EA, Wasserman SM, Dias C, et al. AMG145. Drug Future 2013;38:451-9
   Web of Science ®Google Scholar
• Chan CY, Piper DE, Cao Q, et al. A proprotein convertase subtilisin/kexin type 9 neutralizing antibody reduces serum cholesterol in mice and nonhuman primates. Proc Natl Acad Sci USA 2009;106:9820-5
   PubMed Web of Science ®Google Scholar
• Foltz IN, Karow M, Wasserman SM. Evolution and emergence of therapeutic monoclonal antibodies. What cardiologists need to know. Circulation 2013;127:2222-30
   PubMed Web of Science ®Google Scholar
• Dias CS, Shaywitz AJ, Wasserman SM, et al. Effects of AMG145 on low-density lipoprotein cholesterol levels. Results from 2 randomized, double-blind, placebo-controlled, ascending dose phase 1studies in healthy volunteers and hypercholesterolemic subjects on statins. J Am Coll Cardiol 2012;60:1888-98
   PubMed Web of Science ®Google Scholar
• 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, placebo-controlled, phase 2 study. Lancet 2012;380(9858):1995-2006
   PubMed Web of Science ®Google Scholar
• Kohli P, Desai NR, Giugliano RP, et al. Design and rationale of the LAPLACE-TIMI 57 trial: a phase II, double-blind, placebo-controlled study of the efficacy and tolerability of a monoclonal antibody inhibitor of PCSK9 in subjects with hypercholesterolemia on background statin therapy. Clin Cardiol 2012;35(7):385-91
   PubMed Web of Science ®Google Scholar
• Giugliano RP, Desai NR, Kohli P, et al. Efficacy, safety, and tolerability of a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 in combination with a statin in patients with hypercholesterolaemia (LAPLACE-TIMI 57): a randomised, placebo-controlled, dose-ranging, phase 2 study. Lancet 2012;380(9858):2007-17
   PubMed Web of Science ®Google Scholar
• Desai NR, Kohli P, Giugliano RP, et al. AMG145, a monoclonal antibody against proprotein convertase subtilisin kexin type 9, significantly reduces lipoprotein(a) in hypercholesterolemic patients receiving statin therapy: an analysis from the LDL-C assessment with proprotein convertase subtilisin kexin type 9 monoclonal antibody inhibition combined with statin therapy (LAPLACE)-thrombolysis in myocardial infarction (TIMI) 57 trial. Circulation 2013;128(9):962-9
   PubMed Web of Science ®Google Scholar
• McKenney JM, Koren MJ, Kereiakes DJ, et al. 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 2012;59:2344-53
   PubMed Web of Science ®Google Scholar
• Leigh SE, Foster AH, Whittall RA, et al. Uptake and analysis of the University College London low density lipoprotein receptor familial hypercholesterolemia database. Ann Hum Genet 2008;72:485-98
   PubMed Web of Science ®Google Scholar
• Innerarity TL, Weisgraber KH, Arnold KS, et al. Familial defective apolipoprotein B-100: low density lipoproteins with abnormal receptor binding. Proc Natl Acad Sci USA 1987;84:6919-23
   PubMed Web of Science ®Google Scholar
• Raal F, Scott R, Somaratne R, et al. Low-density lipoprotein cholesterol-lowering effects of AMG 145, a monoclonal antibody to proprotein convertase subtilisin/kexin type 9 serine protease in patients with heterozygous familial hypercholesterolemia: the reduction of LDL-C with PCSK9 inhibition in heterozygous familial hypercholesterolemia disorder (RUTHERFORD) randomized trial. Circulation 2012;126(20):2408-17
   PubMed Web of Science ®Google Scholar
• Stein EA, Gipe D, Bergeron J, et al. Effect of a monoclonal antibody to protein convertase subtilisin/kexin type 9 serine protease, SAR236553/REGN727, in patients with primary hypercholesterolemia receiving ongoing stable atorvastatin therapy. J Am Coll Cardiol 2012;59:2344-53
   PubMed Web of Science ®Google Scholar
• Sullivan D, Olsson AG, Scott R, et al. Effect of a monoclonal antibody to PCSK9 on low-density lipoprotein cholesterol levels in statin-intolerant patients. The GAUSS randomized trial. JAMA 2012;308:2497-506
   PubMed Web of Science ®Google Scholar
• Stein EA, Honarpour N, Wasserman SM, et al. Effect of the proprotein convertase subtilisin/kexin 9 monoclonal antibody, AMG 145, in homozygous familial hypercholesterolemia. Circulation 2013;128(19):2113-20
   PubMed Web of Science ®Google Scholar
• Available from: http://clinicaltrials.gov/show/NCT01439880 [Last Accessed 1 December 2013]
   Google Scholar
• Koren MJ, Giugliano RP, Raal F, et al. Randomized comparison of the safety, tolerability and efficacy of long-term administration of AMG 145 versus standard of care in 1004 patients: 52 week results from the OSLER trial. Circulation 2014;129(2):234-43
   PubMed Web of Science ®Google Scholar
• Available from: http://clinicaltrials.gov/show/NCT01764633 [Last Accessed 1 December 2013]
   Google Scholar
• Available from: http://clinicaltrials.gov/ct2/show/record/NCT01133522 [Last Accessed 1 December 2013]
   Google Scholar
• Gotto AM Jr, Moon JE. Pharmacotherapies for lipid modification: beyond the statins. Nat Rev Cardiol 2013;10:560-70
   PubMed Web of Science ®Google Scholar
• Catapano AL. Perspectives on low-density lipoprotein cholesterol goal achievement. Curr Med Res Opin 2009;25:431-47
   PubMed Web of Science ®Google Scholar
• Jones PH, Nair R, Thakker KM. Prevalence of dyslipidemia and lipid goal attainment in statin-treated subjects from 3 data sources: a retrospective analysis. J Am Heart Assoc 2012;1:e001800
   Web of Science ®Google Scholar
• European Association for Cardiovascular Prevention & Rehabilitation1, Reiner Z, Catapano AL, De Backer G, ESC Committee for Practice Guidelines (CPG) 2008-2010 and 2010-2012 Committees. ESC/EAS guidelines for the management of dyslipidaemias: the task force for the management of dyslipidaemias of the European Society of Cardiology (ESC) and the European Atherosclerosis Society (EAS). Eur Heart J 2011;32(14):1769-818
   Google Scholar
• Stone NJ, Robinson JG, Lichtenstein AH, for the 2013 ACC/AHA Cholesterol Guideline Panel*. Treatment of blood cholesterol to reduce atherosclerotic cardiovascular disease risk in adults: synopsis of the 2013 ACC/AHA cholesterol guideline. Ann Intern Med 2014;160(5):339-43. 343
   PubMed Web of Science ®Google Scholar
• Raal FJ, Giugliano RP, Sabatine MS, et al. Reduction in lipoprotein (a) with the PCSK9 monoclonal antibody evolocumab (AMG 145): a pooled analysis of over 1300 patients in 4 phase 2 trials. J Am Coll Cardiol 2014. [Epub ahead of print]
   PubMed Web of Science ®Google Scholar