Literature DB >> 26702335

How Do PCSK9 Inhibitors Stack Up to Statins for Low-Density Lipoprotein Cholesterol Control?

Marj P Zimmerman1.   

Abstract

Despite advances in the approach toward treating hypercholesterolemia and widespread access to statin medications, not all people are able to reach target low-density lipoprotein cholesterol (LDL-C) levels to reduce their cardiovascular risk. Some of the reasons include the inability to tolerate statin therapy, LDL-C levels that remain high even in the presence of statin therapy, and a familial disorder that is characterized by extremely high levels of LDL-C. A new therapeutic class, proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors, represents a novel and promising approach to reducing LDL-C levels using a mechanism at the LDL receptor level. The recent approval of the first 2 PCSK9 inhibitors and the anticipated approval of the third agent in this class within approximately 1 year may provide clinicians powerful new weapons to lower LDL-C levels in patients who are not satisfactorily managed with statins. However, the results of long-term studies of the ability of these new medications to influence cardiovascular outcomes will not be known for several years.

Entities:  

Keywords:  PCSK9 inhibitors; alirocumab; bococizumab; evolocumab; familial hypercholesterolemia; low-density lipoprotein cholesterol; statin adverse effects; statin treatment

Year:  2015        PMID: 26702335      PMCID: PMC4684634     

Source DB:  PubMed          Journal:  Am Health Drug Benefits        ISSN: 1942-2962


  19 in total

Review 1.  Lipid lowering with PCSK9 inhibitors.

Authors:  Razvan T Dadu; Christie M Ballantyne
Journal:  Nat Rev Cardiol       Date:  2014-06-24       Impact factor: 32.419

2.  Cardiology patient page. Statin intolerance.

Authors:  David H Fitchett; Robert A Hegele; Subodh Verma
Journal:  Circulation       Date:  2015-03-31       Impact factor: 29.690

3.  Effect of the proprotein convertase subtilisin/kexin 9 monoclonal antibody, AMG 145, in homozygous familial hypercholesterolemia.

Authors:  Evan A Stein; Narimon Honarpour; Scott M Wasserman; Feng Xu; Rob Scott; Frederick J Raal
Journal:  Circulation       Date:  2013-09-06       Impact factor: 29.690

4.  A 52-week placebo-controlled trial of evolocumab in hyperlipidemia.

Authors:  Dirk J Blom; Tomas Hala; Michael Bolognese; Michael J Lillestol; Phillip D Toth; Lesley Burgess; Richard Ceska; Eli Roth; Michael J Koren; Christie M Ballantyne; Maria Laura Monsalvo; Kate Tsirtsonis; Jae B Kim; Rob Scott; Scott M Wasserman; Evan A Stein
Journal:  N Engl J Med       Date:  2014-03-29       Impact factor: 91.245

5.  Familial hypercholesterolemia and estimation of US patients eligible for low-density lipoprotein apheresis after maximally tolerated lipid-lowering therapy.

Authors:  Raghu Vishwanath; Linda C Hemphill
Journal:  J Clin Lipidol       Date:  2013-11-08       Impact factor: 4.766

6.  Monotherapy with the PCSK9 inhibitor alirocumab versus ezetimibe in patients with hypercholesterolemia: results of a 24 week, double-blind, randomized Phase 3 trial.

Authors:  Eli M Roth; Marja-Riitta Taskinen; Henry N Ginsberg; John J P Kastelein; Helen M Colhoun; Jennifer G Robinson; Laurence Merlet; Robert Pordy; Marie T Baccara-Dinet
Journal:  Int J Cardiol       Date:  2014-07-02       Impact factor: 4.164

7.  Inhibition of PCSK9 with evolocumab in homozygous familial hypercholesterolaemia (TESLA Part B): a randomised, double-blind, placebo-controlled trial.

Authors:  Frederick J Raal; Narimon Honarpour; Dirk J Blom; G Kees Hovingh; Feng Xu; Rob Scott; Scott M Wasserman; Evan A Stein
Journal:  Lancet       Date:  2014-10-01       Impact factor: 79.321

8.  Anti-PCSK9 antibody effectively lowers cholesterol in patients with statin intolerance: the GAUSS-2 randomized, placebo-controlled phase 3 clinical trial of evolocumab.

Authors:  Erik Stroes; David Colquhoun; David Sullivan; Fernando Civeira; Robert S Rosenson; Gerald F Watts; Eric Bruckert; Leslie Cho; Ricardo Dent; Beat Knusel; Allen Xue; Rob Scott; Scott M Wasserman; Michael Rocco
Journal:  J Am Coll Cardiol       Date:  2014-03-30       Impact factor: 24.094

9.  Efficacy and safety of alirocumab in high cardiovascular risk patients with inadequately controlled hypercholesterolaemia on maximally tolerated doses of statins: the ODYSSEY COMBO II randomized controlled trial.

Authors:  Christopher P Cannon; Bertrand Cariou; Dirk Blom; James M McKenney; Christelle Lorenzato; Robert Pordy; Umesh Chaudhari; Helen M Colhoun
Journal:  Eur Heart J       Date:  2015-02-16       Impact factor: 29.983

10.  Elevated PCSK9 levels in untreated patients with heterozygous or homozygous familial hypercholesterolemia and the response to high-dose statin therapy.

Authors:  Frederick Raal; Vanessa Panz; Andrew Immelman; Gillian Pilcher
Journal:  J Am Heart Assoc       Date:  2013-04-24       Impact factor: 5.501

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  10 in total

1.  Formulation and Characterization of Phytostanol Ester Solid Lipid Nanoparticles for the Management of Hypercholesterolemia: An ex vivo Study.

Authors:  Sony Chandi Shrestha; Kebreab Ghebremeskel; Kenneth White; Caterina Minelli; Ihab Tewfik; Panna Thapa; Sundus Tewfik
Journal:  Int J Nanomedicine       Date:  2021-03-09

2.  Eligibility for alirocumab or evolocumab treatment in 1090 hypercholesterolemic patients referred to a regional cholesterol treatment center with LDL cholesterol ≥70 mg/dL despite maximal-tolerated LDL-cholesterol-lowering therapy.

Authors:  Vybhav Jetty; Charles J Glueck; Kevin Lee; Naila Goldenberg; Marloe Prince; Ashwin Kumar; Michael Goldenberg; Ishan Anand; Ping Wang
Journal:  Vasc Health Risk Manag       Date:  2017-07-06

3.  Statin use reduces cardiovascular events and all-cause mortality amongst Chinese patients with type 2 diabetes mellitus: a 5-year cohort study.

Authors:  Colman Siu Cheung Fung; Eric Yuk Fai Wan; Anca Ka Chun Chan; Cindy Lo Kuen Lam
Journal:  BMC Cardiovasc Disord       Date:  2017-06-24       Impact factor: 2.298

4.  A Genomic DNA Reporter Screen Identifies Squalene Synthase Inhibitors That Act Cooperatively with Statins to Upregulate the Low-Density Lipoprotein Receptor.

Authors:  Alastair G Kerr; Lawrence C S Tam; Ashley B Hale; Milena Cioroch; Gillian Douglas; Sarina Agkatsev; Olivia Hibbitt; Joseph Mason; James Holt-Martyn; Carole J R Bataille; Graham M Wynne; Keith M Channon; Angela J Russell; Richard Wade-Martins
Journal:  J Pharmacol Exp Ther       Date:  2017-03-30       Impact factor: 4.030

Review 5.  Management of Statin Intolerance in 2018: Still More Questions Than Answers.

Authors:  Peter P Toth; Angelo Maria Patti; Rosaria Vincenza Giglio; Dragana Nikolic; Giuseppa Castellino; Manfredi Rizzo; Maciej Banach
Journal:  Am J Cardiovasc Drugs       Date:  2018-06       Impact factor: 3.571

6.  Safety and efficacy of alirocumab: A meta analysis of 12 randomized controlled trials.

Authors:  Ajay K Shukla; Rekha Mehani
Journal:  J Family Med Prim Care       Date:  2019-07

7.  CRISPR-Cas12a delivery by DNA-mediated bioresponsive editing for cholesterol regulation.

Authors:  Wujin Sun; Jinqiang Wang; Quanyin Hu; Xingwu Zhou; Ali Khademhosseini; Zhen Gu
Journal:  Sci Adv       Date:  2020-05-20       Impact factor: 14.136

8.  Serum sdLDL-C and Cellular SREBP2-dependent Cholesterol Levels; is there a Challenge on Targeting PCSK9?

Authors:  Elham Soltanmohammadi; Sadegh Piran; Asghar Mohammadi; Bita Hosseni; Faezeh Naseri; Mohammad Shabani; Mohammad Najafi
Journal:  J Med Biochem       Date:  2016-11-02       Impact factor: 3.402

9.  American Association of Clinical Endocrinologists/American College of Endocrinology Management of Dyslipidemia and Prevention of Cardiovascular Disease Clinical Practice Guidelines.

Authors:  Paul S Jellinger
Journal:  Diabetes Spectr       Date:  2018-08

10.  The Cholesterol-Modulating Effect of Methanol Extract of Pigeon Pea (Cajanus cajan (L.) Millsp.) Leaves on Regulating LDLR and PCSK9 Expression in HepG2 Cells.

Authors:  Heng-Yuan Chang; Jia-Ru Wu; Wan-Yun Gao; Huei-Ru Lin; Pei-Yi Chen; Chen-I Chen; Ming-Jiuan Wu; Jui-Hung Yen
Journal:  Molecules       Date:  2019-01-30       Impact factor: 4.411

  10 in total

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