Literature DB >> 25037695

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

Eli M Roth1, Marja-Riitta Taskinen2, Henry N Ginsberg3, John J P Kastelein4, Helen M Colhoun5, Jennifer G Robinson6, Laurence Merlet7, Robert Pordy8, Marie T Baccara-Dinet9.   

Abstract

BACKGROUND: Efficacy and safety of alirocumab were compared with ezetimibe in hypercholesterolemic patients at moderate cardiovascular risk not receiving statins or other lipid-lowering therapy.
METHODS: In a Phase 3, randomized, double-blind, double-dummy study (NCT01644474), patients (low-density lipoprotein cholesterol [LDL-C] 100-190 mg/dL, 10-year risk of fatal cardiovascular events ≥ 1%-<5% [systemic coronary risk estimation]) were randomized to ezetimibe 10mg/day (n=51) or alirocumab 75 mg subcutaneously (via 1-mL autoinjector) every 2 weeks (Q2W) (n=52), with dose up-titrated to 150 mg Q2W (also 1 mL) at week 12 if week 8 LDL-C was ≥ 70 mg/dL. Primary endpoint was mean LDL-C % change from baseline to 24 weeks, analyzed using all available data (intent-to-treat approach, ITT). Analyses using on-treatment LDL-C values were also conducted.
RESULTS: Mean (SD) baseline LDL-C levels were 141.1 (27.1) mg/dL (alirocumab) and 138.3 (24.5) mg/dL (ezetimibe). The 24-week treatment period was completed by 85% of alirocumab and 86% of ezetimibe patients. Least squares mean (SE) LDL-C reductions were 47 (3)% with alirocumab versus 16 (3)% with ezetimibe (ITT; p<0.0001) and 54 (2)% versus 17 (2)% (on-treatment; p<0.0001). At week 12, before up-titration, alirocumab 75 mg Q2W reduced LDL-C by 53 (2)% (on-treatment). Injection site reactions were infrequent (<2% and <4% of alirocumab and ezetimibe patients, respectively).
CONCLUSIONS: Alirocumab demonstrated significantly greater LDL-C lowering versus ezetimibe after 24 weeks with the lower 75 mg Q2W dose sufficient to provide ≥ 50% LDL-C reduction in the majority of the patients. Adverse events were comparable between groups.
Copyright © 2014. Published by Elsevier Ireland Ltd.

Entities:  

Keywords:  Alirocumab; Cholesterol-lowering drugs; Hypercholesterolemia; LDL-C; Monoclonal antibodies; PCSK9

Mesh:

Substances:

Year:  2014        PMID: 25037695     DOI: 10.1016/j.ijcard.2014.06.049

Source DB:  PubMed          Journal:  Int J Cardiol        ISSN: 0167-5273            Impact factor:   4.164


  75 in total

Review 1.  Low Density Lipoprotein (LDL) Cholesterol as a Causal Role for Atherosclerotic Disease: Potential Role of PCSK9 Inhibitors.

Authors:  Rita Del Pinto; Davide Grassi; Giuliana Properzi; Giovambattista Desideri; Claudio Ferri
Journal:  High Blood Press Cardiovasc Prev       Date:  2019-06-24

Review 2.  Alirocumab as add-on therapy to statins: current evidence and clinical potential.

Authors:  Johann Auer; Robert Berent
Journal:  Ther Adv Cardiovasc Dis       Date:  2018-05-24

Review 3.  PCSK9 inhibitors for treating dyslipidemia in patients at different cardiovascular risk: a systematic review and a meta-analysis.

Authors:  Alessandro Squizzato; Matteo Basilio Suter; Marta Nerone; Robert Patrick Giugliano; Francesco Dentali; Andrea Maria Maresca; Leonardo Campiotti; Anna Maria Grandi; Luigina Guasti
Journal:  Intern Emerg Med       Date:  2017-07-10       Impact factor: 3.397

4.  Alirocumab as Add-On to Atorvastatin Versus Other Lipid Treatment Strategies: ODYSSEY OPTIONS I Randomized Trial.

Authors:  Harold Bays; Daniel Gaudet; Robert Weiss; Juan Lima Ruiz; Gerald F Watts; Ioanna Gouni-Berthold; Jennifer Robinson; Jian Zhao; Corinne Hanotin; Stephen Donahue
Journal:  J Clin Endocrinol Metab       Date:  2015-06-01       Impact factor: 5.958

Review 5.  Future Lipid-Altering Therapeutic Options Targeting Residual Cardiovascular Risk.

Authors:  Michel Farnier
Journal:  Curr Cardiol Rep       Date:  2016-07       Impact factor: 2.931

6.  Population Pharmacokinetics (PK) and Pharmacodynamics (PD) Analysis of LY3015014, a Monoclonal Antibody to Protein Convertase Subtilisin/Kexin Type 9 (PCSK9) in Healthy Subjects and Hypercholesterolemia Patients.

Authors:  Tong Shen; Douglas E James; Kathryn A Krueger
Journal:  Pharm Res       Date:  2016-11-07       Impact factor: 4.200

Review 7.  The Emerging Role of PCSK9 Inhibitors in Preventive Cardiology.

Authors:  Reynaria N Pitts; Robert H Eckel
Journal:  Eur Cardiol       Date:  2014-12

Review 8.  Alirocumab: First Global Approval.

Authors:  Anthony Markham
Journal:  Drugs       Date:  2015-09       Impact factor: 9.546

Review 9.  PCSK9 Mutations in Familial Hypercholesterolemia: from a Groundbreaking Discovery to Anti-PCSK9 Therapies.

Authors:  Petra El Khoury; Sandy Elbitar; Youmna Ghaleb; Yara Abou Khalil; Mathilde Varret; Catherine Boileau; Marianne Abifadel
Journal:  Curr Atheroscler Rep       Date:  2017-10-17       Impact factor: 5.113

Review 10.  Antibodies to watch in 2015.

Authors:  Janice M Reichert
Journal:  MAbs       Date:  2015       Impact factor: 5.857

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