Targeting PCSK9 for Therapeutic Gains

Efficacy and Safety of Alirocumab as Add-on Therapy in High-Cardiovascular-Risk Patients With Hypercholesterolemia Not Adequately Controlled With Atorvastatin (20 or 40 mg) or Rosuvastatin (10 or 20 mg): Design and Rationale of the ODYSSEY OPTIONS Studies

(2015) Jennifer G. Robinson et al.   CLINICAL CARDIOLOGY

Effect of alirocumab, a monoclonal antibody to PCSK9, on long-term cardiovascular outcomes following acute coronary syndromes: Rationale and design of the ODYSSEY Outcomes trial

(2014) Gregory G. Schwartz et al.   AMERICAN HEART JOURNAL

Effect of Alirocumab, a Monoclonal Proprotein Convertase Subtilisin/Kexin 9 Antibody, on Lipoprotein(a) Concentrations (a Pooled Analysis of 150 mg Every Two Weeks Dosing from Phase 2 Trials)

(2014) Daniel Gaudet et al.   AMERICAN JOURNAL OF CARDIOLOGY

Efficacy and safety of alirocumab, a fully human PCSK9 monoclonal antibody, in high cardiovascular risk patients with poorly controlled hypercholesterolemia on maximally tolerated doses of statins: rationale and design of the ODYSSEY COMBO I and II trials

(2014) Helen M Colhoun et al.   BMC Cardiovascular Disorders

Antihyperlipidemic Therapies Targeting PCSK9

(2014) Michael Weinreich et al.   Cardiology in Review

Efficacy and Safety of Alirocumab in Patients with Heterozygous Familial Hypercholesterolemia not Adequately Controlled with Current Lipid-Lowering Therapy: Design and Rationale of the ODYSSEY FH Studies

(2014) John J. P. Kastelein et al.   CARDIOVASCULAR DRUGS AND THERAPY

Proprotein Convertase Subtilisin Kexin Type 9 Promotes Intestinal Overproduction of Triglyceride-Rich Apolipoprotein B Lipoproteins Through Both Low-Density Lipoprotein Receptor–Dependent and –Independent Mechanisms

(2014) Shirya Rashid et al.   CIRCULATION

Living the PCSK9 Adventure: from the Identification of a New Gene in Familial Hypercholesterolemia Towards a Potential New Class of Anticholesterol Drugs

(2014) Marianne Abifadel et al.   Current Atherosclerosis Reports

Effect of Evolocumab or Ezetimibe Added to Moderate- or High-Intensity Statin Therapy on LDL-C Lowering in Patients With Hypercholesterolemia

(2014) Jennifer G. Robinson et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Efficacy and safety of alirocumab, a monoclonal antibody to PCSK9, in statin-intolerant patients: Design and rationale of ODYSSEY ALTERNATIVE, a randomized phase 3 trial

(2014) Patrick M. Moriarty et al.   Journal of Clinical Lipidology

An assessment by the Statin Intolerance Panel: 2014 update

(2014) John R. Guyton et al.   Journal of Clinical Lipidology

Anti-PCSK9 Antibody Effectively Lowers Cholesterol in Patients With Statin Intolerance

(2014) Erik Stroes et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Anti-PCSK9 Monotherapy for Hypercholesterolemia

(2014) Michael J. Koren et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Reduction in Lipoprotein(a) With PCSK9 Monoclonal Antibody Evolocumab (AMG 145)

(2014) Frederick J. Raal et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Lipid lowering with PCSK9 inhibitors

(2014) Razvan T. Dadu et al.   Nature Reviews Cardiology

A 52-Week Placebo-Controlled Trial of Evolocumab in Hyperlipidemia

(2014) Dirk J. Blom et al.   NEW ENGLAND JOURNAL OF MEDICINE

PCSK9 plays a significant role in cholesterol homeostasis and lipid transport in intestinal epithelial cells

(2013) Emile Levy et al.   ATHEROSCLEROSIS

Effect of the Proprotein Convertase Subtilisin/Kexin 9 Monoclonal Antibody, AMG 145, in Homozygous Familial Hypercholesterolemia

(2013) Evan A. Stein et al.   CIRCULATION

Serum Proprotein Convertase Subtilisin/Kexin Type 9 and Cell Surface Low-Density Lipoprotein Receptor

(2013) Hagai Tavori et al.   CIRCULATION

Loss of Plasma Proprotein Convertase Subtilisin/Kexin 9 (PCSK9) After Lipoprotein Apheresis

(2013) Hagai Tavori et al.   CIRCULATION RESEARCH

HPS2-THRIVE randomized placebo-controlled trial in 25 673 high-risk patients of ER niacin/laropiprant: trial design, pre-specified muscle and liver outcomes, and reasons for stopping study treatment

(2013) et al.   EUROPEAN HEART JOURNAL

Low Density Lipoprotein Binds to Proprotein Convertase Subtilisin/Kexin Type-9 (PCSK9) in Human Plasma and Inhibits PCSK9-mediated Low Density Lipoprotein Receptor Degradation

(2013) Tanja Kosenko et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Relationship of Apolipoproteins A-1 and B, and Lipoprotein(a) to Cardiovascular Outcomes

(2013) John J. Albers et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Effect of an RNA interference drug on the synthesis of proprotein convertase subtilisin/kexin type 9 (PCSK9) and the concentration of serum LDL cholesterol in healthy volunteers: a randomised, single-blind, placebo-controlled, phase 1 trial

(2013) Kevin Fitzgerald et al.   LANCET

RNAi targeting PCSK9 decreases lipid levels in a human trial

(2013) Megan Cully   Nature Reviews Cardiology

Proprotein Convertase Subtilisin/Kexin Type 9 Interacts With Apolipoprotein B and Prevents Its Intracellular Degradation, Irrespective of the Low-Density Lipoprotein Receptor

(2012) Hua Sun et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Homozygous familial hypercholesterolemia: Current perspectives on diagnosis and treatment

(2012) Frederick J. Raal et al.   ATHEROSCLEROSIS

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

(2012) Frederick Raal et al.   CIRCULATION

Apolipoprotein B Synthesis Inhibition With Mipomersen in Heterozygous Familial Hypercholesterolemia

(2012) Evan A. Stein et al.   CIRCULATION

Effect of a Monoclonal Antibody to PCSK9 on Low-Density Lipoprotein Cholesterol Levels in Statin-Intolerant Patients

(2012) David Sullivan et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Effects of AMG 145 on Low-Density Lipoprotein Cholesterol Levels

(2012) Clapton S. Dias et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

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

(2012) James M. McKenney et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

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

(2012) Michael J Koren et al.   LANCET

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

(2012) Robert P Giugliano et al.   LANCET

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

(2012) Evan A Stein et al.   LANCET

Effect of a Monoclonal Antibody to PCSK9 on LDL Cholesterol

(2012) Evan A. Stein et al.   NEW ENGLAND JOURNAL OF MEDICINE

Atorvastatin with or without an Antibody to PCSK9 in Primary Hypercholesterolemia

(2012) Eli M. Roth et al.   NEW ENGLAND JOURNAL OF MEDICINE

Circulating Proprotein Convertase Subtilisin/Kexin 9 (PCSK9) Regulates VLDLR Protein and Triglyceride Accumulation in Visceral Adipose Tissue

(2011) Anna Roubtsova et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Niacin in Patients with Low HDL Cholesterol Levels Receiving Intensive Statin Therapy

(2011)   NEW ENGLAND JOURNAL OF MEDICINE

Proprotein Convertase Subtilisin Kexin Type 9 Null Mice Are Protected From Postprandial Triglyceridemia

(2009) Cédric Le May et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Proprotein convertase subtilisin/kexin type 9 (PCSK9): Hepatocyte-specific low-density lipoprotein receptor degradation and critical role in mouse liver regeneration

(2008) Ahmed Zaid et al.   HEPATOLOGY