PCSK9 inhibition 2018: riding a new wave of coronary prevention

PCSK9 Inhibitors: Mechanisms of Action, Metabolic Effects, and Clinical Outcomes

(2018) Connie N. Hess et al.   Annual Review of Medicine

Efficacy and safety of alirocumab in patients with or without prior coronary revascularization: Pooled analysis of eight ODYSSEY phase 3 trials

(2018) Dean J. Kereiakes et al.   ATHEROSCLEROSIS

Proprotein Convertase Subtilisin Kexin 9 Inhibitors

(2018) Angela Pirillo et al.   CARDIOLOGY CLINICS

Clinical Benefit of Evolocumab by Severity and Extent of Coronary Artery Disease: An Analysis from FOURIER

(2018) Marc S. Sabatine et al.   CIRCULATION

Effect of an siRNA Therapeutic Targeting PCSK9 on Atherogenic Lipoproteins: Pre-Specified Secondary End Points in ORION 1

(2018) Kausik K. Ray et al.   CIRCULATION

Controlled study of the effect of proprotein convertase subtilisin-kexin type 9 inhibition with evolocumab on lipoprotein(a) particle kinetics

(2018) Gerald F Watts et al.   EUROPEAN HEART JOURNAL

Estimated individual lifetime benefit from PCSK9 inhibition in statin-treated patients with coronary artery disease

(2018) Lotte Kaasenbrood et al.   HEART

The cost-effectiveness of PCSK9 inhibitors - The Australian healthcare perspective

(2018) Radya Kumar et al.   INTERNATIONAL JOURNAL OF CARDIOLOGY

Alirocumab efficacy in patients with double heterozygous, compound heterozygous, or homozygous familial hypercholesterolemia

(2018) Merel L. Hartgers et al.   Journal of Clinical Lipidology

Alirocumab in high-risk patients: Observations from the open-label expanded use program

(2018) Charles J. Glueck et al.   Journal of Clinical Lipidology

Improved endothelial function after short-term therapy with evolocumab

(2018) Guglielmo Maulucci et al.   Journal of Clinical Lipidology

PCSK9 and neurocognitive function: Should it be still an issue after FOURIER and EBBINGHAUS results?

(2018) Massimo R. Mannarino et al.   Journal of Clinical Lipidology

Cardiovascular event reduction with PCSK9 inhibition among 1578 patients with familial hypercholesterolemia: Results from the SPIRE randomized trials of bococizumab

(2018) Paul M Ridker et al.   Journal of Clinical Lipidology

Generation and Characterization of a Novel Small Biologic Alternative to Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Antibodies, DS-9001a, Albumin Binding Domain–Fused Anticalin Protein

(2018) Yusuke Masuda et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Advances in lipid-lowering therapy through gene-silencing technologies

(2018) Børge G. Nordestgaard et al.   Nature Reviews Cardiology

Development of vaccine for dyslipidemia targeted to a proprotein convertase subtilisin/kexin type 9 (PCSK9) epitope in mice

(2018) Ryo Kawakami et al.   PLoS One

PCSK9 induces a pro-inflammatory response in macrophages

(2018) Chiara Ricci et al.   Scientific Reports

Persistent Safety and Efficacy of Evolocumab in Patients with Statin Intolerance: a Subset Analysis of the OSLER Open-Label Extension Studies

(2018) Leslie Cho et al.   CARDIOVASCULAR DRUGS AND THERAPY

Lipoprotein(a) and secondary prevention of atherothrombotic events: A critical appraisal

(2018) Michael B. Boffa et al.   Journal of Clinical Lipidology

Efficacy and Safety of Further Lowering of Low-Density Lipoprotein Cholesterol in Patients Starting With Very Low Levels

(2018) Marc S. Sabatine et al.   JAMA Cardiology

Effect of Evolocumab on Coronary Plaque Composition

(2018) Stephen J. Nicholls et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Alirocumab Reduces Fatal and Nonfatal Cardiovascular Events

(2018) Michael Szarek et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Alirocumab and Cardiovascular Outcomes after Acute Coronary Syndrome

(2018) Gregory G. Schwartz et al.   NEW ENGLAND JOURNAL OF MEDICINE

Low-Dose Methotrexate for the Prevention of Atherosclerotic Events

(2018) Paul M Ridker et al.   NEW ENGLAND JOURNAL OF MEDICINE

No evidence of neurocognitive adverse events associated with alirocumab treatment in 3340 patients from 14 randomized Phase 2 and 3 controlled trials: a meta-analysis of individual patient data

(2017) Philip D Harvey et al.   EUROPEAN HEART JOURNAL

Low-density lipoproteins cause atherosclerotic cardiovascular disease. 1. Evidence from genetic, epidemiologic, and clinical studies. A consensus statement from the European Atherosclerosis Society Consensus Panel

(2017) Brian A. Ference et al.   EUROPEAN HEART JOURNAL

2017 Update of ESC/EAS Task Force on practical clinical guidance for proprotein convertase subtilisin/kexin type 9 inhibition in patients with atherosclerotic cardiovascular disease or in familial hypercholesterolaemia

(2017) Ulf Landmesser et al.   EUROPEAN HEART JOURNAL

The AT04A vaccine against proprotein convertase subtilisin/kexin type 9 reduces total cholesterol, vascular inflammation, and atherosclerosis in APOE*3Leiden.CETP mice

(2017) Christine Landlinger et al.   EUROPEAN HEART JOURNAL

PCSK9 and Atherosclerosis - Lipids and Beyond

(2017) Michael D. Shapiro et al.   Journal of Atherosclerosis and Thrombosis

PCSK9 at the crossroad of cholesterol metabolism and immune function during infections

(2017) Francesco Paciullo et al.   JOURNAL OF CELLULAR PHYSIOLOGY

Long-term safety, tolerability, and efficacy of evolocumab in patients with heterozygous familial hypercholesterolemia

(2017) G. Kees Hovingh et al.   Journal of Clinical Lipidology

The PCSK9-LDL Receptor Axis and Outcomes in Heart Failure

(2017) Antoni Bayes-Genis et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

PCSK9 Inhibitors

(2017) Mark A. Hlatky et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Clinical efficacy and safety of achieving very low LDL-cholesterol concentrations with the PCSK9 inhibitor evolocumab: a prespecified secondary analysis of the FOURIER trial

(2017) Robert P Giugliano et al.   LANCET

Nine paths to PCSK9 inhibition

(2017) Asher Mullard   NATURE REVIEWS DRUG DISCOVERY

Evolocumab and Clinical Outcomes in Patients with Cardiovascular Disease

(2017) Marc S. Sabatine et al.   NEW ENGLAND JOURNAL OF MEDICINE

A Highly Durable RNAi Therapeutic Inhibitor of PCSK9

(2017) Kevin Fitzgerald et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inclisiran in Patients at High Cardiovascular Risk with Elevated LDL Cholesterol

(2017) Kausik K. Ray et al.   NEW ENGLAND JOURNAL OF MEDICINE

Cardiovascular Efficacy and Safety of Bococizumab in High-Risk Patients

(2017) Paul M Ridker et al.   NEW ENGLAND JOURNAL OF MEDICINE

Antiinflammatory Therapy with Canakinumab for Atherosclerotic Disease

(2017) Paul M Ridker et al.   NEW ENGLAND JOURNAL OF MEDICINE

Budget Impact Analysis of PCSK9 Inhibitors for the Management of Adult Patients with Heterozygous Familial Hypercholesterolemia or Clinical Atherosclerotic Cardiovascular Disease

(2017) Usha G. Mallya et al.   PHARMACOECONOMICS

Regulation of PCSK9 by nutraceuticals

(2017) Amir Abbas Momtazi et al.   PHARMACOLOGICAL RESEARCH

PCSK9 deficiency results in increased ectopic fat accumulation in experimental models and in humans

(2017) Andrea Baragetti et al.   European Journal of Preventive Cardiology

Effect of PCSK9 Inhibitors on Clinical Outcomes in Patients With Hypercholesterolemia: A Meta‐Analysis of 35 Randomized Controlled Trials

(2017) Aris Karatasakis et al.   Journal of the American Heart Association

Vaccine against PCSK9: the natural strategy from passive to active immunization for the prevention of atherosclerosis

(2017) Fernando Civeira et al.   Journal of Thoracic Disease

Lipoprotein(a) and inhibitors of proprotein convertase subtilisin/kexin type 9

(2017) Kazuhiko Kotani et al.   Journal of Thoracic Disease

Long-term treatment with evolocumab added to conventional drug therapy, with or without apheresis, in patients with homozygous familial hypercholesterolaemia: an interim subset analysis of the open-label TAUSSIG study

(2017) Frederick J Raal et al.   Lancet Diabetes & Endocrinology

Cardiovascular safety and efficacy of the PCSK9 inhibitor evolocumab in patients with and without diabetes and the effect of evolocumab on glycaemia and risk of new-onset diabetes: a prespecified analysis of the FOURIER randomised controlled trial

(2017) Marc S Sabatine et al.   Lancet Diabetes & Endocrinology

Updated Cost-effectiveness Assessments of PCSK9 Inhibitors From the Perspectives of the Health System and Private Payers

(2017) Alejandro Arrieta et al.   JAMA Cardiology

Homozygous Familial Hypercholesterolemia Patients With Identical Mutations Variably Express the LDLR (Low-Density Lipoprotein Receptor)

(2017) Aurélie Thedrez et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Low-Density Lipoprotein Cholesterol Lowering With Evolocumab and Outcomes in Patients With Peripheral Artery Disease

(2017) Marc P. Bonaca et al.   CIRCULATION

A Therapeutic Peptide Vaccine Against PCSK9

(2017) Yajie Pan et al.   Scientific Reports

Biology of proprotein convertase subtilisin kexin 9: beyond low-density lipoprotein cholesterol lowering

(2016) Giuseppe Danilo Norata et al.   CARDIOVASCULAR RESEARCH

Circulating Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Predicts Future Risk of Cardiovascular Events Independently of Established Risk FactorsCLINICAL PERSPECTIVE

(2016) Karin Leander et al.   CIRCULATION

Effects of PCSK9 Inhibition With Alirocumab on Lipoprotein Metabolism in Healthy HumansClinical Perspective

(2016) Gissette Reyes-Soffer et al.   CIRCULATION

Factorial Effects of Evolocumab and Atorvastatin on Lipoprotein MetabolismClinical Perspective

(2016) Gerald F. Watts et al.   CIRCULATION

PCSK9 Association With Lipoprotein(a)Novelty and Significance

(2016) Hagai Tavori et al.   CIRCULATION RESEARCH

ODYSSEY ESCAPE: is PCSK9 inhibition the Trojan Horse for the use of lipoprotein apheresis in familial hypercholesterolaemia?

(2016) Gerald F. Watts et al.   EUROPEAN HEART JOURNAL

Alirocumab in patients with heterozygous familial hypercholesterolaemia undergoing lipoprotein apheresis: the ODYSSEY ESCAPE trial

(2016) Patrick M. Moriarty et al.   EUROPEAN HEART JOURNAL

Association Between Lowering LDL-C and Cardiovascular Risk Reduction Among Different Therapeutic Interventions

(2016) Michael G. Silverman et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Effect of Evolocumab on Progression of Coronary Disease in Statin-Treated Patients

(2016) Stephen J. Nicholls et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Cost-effectiveness of PCSK9 Inhibitor Therapy in Patients With Heterozygous Familial Hypercholesterolemia or Atherosclerotic Cardiovascular Disease

(2016) Dhruv S. Kazi et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Efficacy and Tolerability of Evolocumab vs Ezetimibe in Patients With Muscle-Related Statin Intolerance

(2016) Steven E. Nissen et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Reduction in Total Cardiovascular Events With Ezetimibe/Simvastatin Post-Acute Coronary Syndrome

(2016) Sabina A. Murphy et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Marine n-3 polyunsaturated fatty acids lower plasma proprotein convertase subtilisin kexin type 9 levels in pre- and postmenopausal women: A randomised study

(2016) Christina B. Graversen et al.   VASCULAR PHARMACOLOGY

Defining severe familial hypercholesterolaemia and the implications for clinical management: a consensus statement from the International Atherosclerosis Society Severe Familial Hypercholesterolemia Panel

(2016) Raul D Santos et al.   Lancet Diabetes & Endocrinology

PCSK9-deficiency does not alter blood pressure and sodium balance in mouse models of hypertension

(2015) Jean-Mathieu Berger et al.   ATHEROSCLEROSIS

Cross-talk between LOX-1 and PCSK9 in vascular tissues

(2015) Zufeng Ding et al.   CARDIOVASCULAR RESEARCH

Proprotein Convertase Subtilisin/Kexin Type 9 Inhibition

(2015) Nathalie Bergeron et al.   CIRCULATION

The Agenda for Familial Hypercholesterolemia

(2015) Samuel S. Gidding et al.   CIRCULATION

Recent advances in the understanding and care of familial hypercholesterolaemia: significance of the biology and therapeutic regulation of proprotein convertase subtilisin/kexin type 9

(2015) Michael M. Page et al.   CLINICAL SCIENCE

Statin intolerance

(2015) Ulrich Laufs et al.   CURRENT OPINION IN LIPIDOLOGY

ODYSSEY FH I and FH II: 78 week results with alirocumab treatment in 735 patients with heterozygous familial hypercholesterolaemia

(2015) John J.P. Kastelein et al.   EUROPEAN HEART JOURNAL

Evolocumab in the treatment of dyslipidemia: pre-clinical and clinical pharmacology

(2015) Michael M Page et al.   Expert Opinion on Drug Metabolism & Toxicology

Efficacy and safety of alirocumab vs ezetimibe in statin-intolerant patients, with a statin rechallenge arm: The ODYSSEY ALTERNATIVE randomized trial

(2015) Patrick M. Moriarty et al.   Journal of Clinical Lipidology

Current therapies for lowering lipoprotein (a)

(2015) Julian C. van Capelleveen et al.   JOURNAL OF LIPID RESEARCH

Local effects of human PCSK9 on the atherosclerotic lesion

(2015) Ilaria Giunzioni et al.   JOURNAL OF PATHOLOGY

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

(2015) Frederick J Raal et al.   LANCET

PCSK9 inhibition with evolocumab (AMG 145) in heterozygous familial hypercholesterolaemia (RUTHERFORD-2): a randomised, double-blind, placebo-controlled trial

(2015) Frederick J Raal et al.   LANCET

The Effects of Estrogen on Serum Level and Hepatocyte Expression of PCSK9

(2015) Wen Guo et al.   METABOLISM-CLINICAL AND EXPERIMENTAL

Efficacy and Safety of Evolocumab in Reducing Lipids and Cardiovascular Events

(2015) Marc S. Sabatine et al.   NEW ENGLAND JOURNAL OF MEDICINE

Ezetimibe Added to Statin Therapy after Acute Coronary Syndromes

(2015) Christopher P. Cannon et al.   NEW ENGLAND JOURNAL OF MEDICINE

PCSK9

(2014) Nabil G. Seidah et al.   CIRCULATION RESEARCH

The effect of insulin on circulating PCSK9 in postmenopausal obese women

(2014) Zuhier Awan et al.   CLINICAL BIOCHEMISTRY

Statin myopathy: the fly in the ointment for the prevention of cardiovascular disease in the 21st century?

(2014) Helen I Keen et al.   Expert Opinion On Drug Safety

Influence of physiological changes in endogenous estrogen on circulating PCSK9 and LDL cholesterol

(2014) Moumita Ghosh et al.   JOURNAL OF LIPID RESEARCH

PCSK9 inhibition fails to alter hepatic LDLR, circulating cholesterol, and atherosclerosis in the absence of ApoE

(2014) Brandon Ason et al.   JOURNAL OF LIPID RESEARCH

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

Liver X receptors in lipid metabolism: opportunities for drug discovery

(2014) Cynthia Hong et al.   NATURE REVIEWS DRUG DISCOVERY

Targeting PCSK9 for Hypercholesterolemia

(2013) Giuseppe Danilo Norata et al.   Annual Review of Pharmacology and Toxicology

AMG 145, a Monoclonal Antibody Against PCSK9, Facilitates Achievement of National Cholesterol Education Program–Adult Treatment Panel III Low-Density Lipoprotein Cholesterol Goals Among High-Risk Patients

(2013) Nihar R. Desai 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

Plasma PCSK9 concentrations during an oral fat load and after short term high-fat, high-fat high-protein and high-fructose diets

(2013) Bertrand Cariou et al.   Nutrition & Metabolism

Low-Density Lipoprotein Cholesterol, Apolipoprotein B, and Risk of Coronary Heart Disease: From Familial Hyperlipidemia to Genomics

(2012) C. C. Imes et al.   Biological Research for Nursing

PCSK9 regulates neuronal apoptosis by adjusting ApoER2 levels and signaling

(2012) Kai Kysenius et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Gene Inactivation of Proprotein Convertase Subtilisin/Kexin Type 9 Reduces Atherosclerosis in Mice

(2012) Maxime Denis et al.   CIRCULATION

Regulation of Epithelial Sodium Channel Trafficking by Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9)

(2012) Vikas Sharotri et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

Endogenous Estrogens Lower Plasma PCSK9 and LDL Cholesterol But Not Lp(a) or Bile Acid Synthesis in Women

(2011) Lena Persson et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Proprotein convertase subtilisin kexin type 9 (PCSK9) secreted by cultured smooth muscle cells reduces macrophages LDLR levels

(2011) Nicola Ferri et al.   ATHEROSCLEROSIS

PCSK9 reduces the protein levels of the LDL receptor in mouse brain during development and after ischemic stroke

(2011) Estelle Rousselet et al.   JOURNAL OF LIPID RESEARCH

PCSK9 is not involved in the degradation of LDL receptors and BACE1 in the adult mouse brain

(2010) Mali Liu et al.   JOURNAL OF LIPID RESEARCH

High-dose atorvastatin causes a rapid sustained increase in human serum PCSK9 and disrupts its correlation with LDL cholesterol

(2010) Greg Welder et al.   JOURNAL OF LIPID RESEARCH

PCSK9 is expressed in pancreatic δ-cells and does not alter insulin secretion

(2009) Cédric Langhi et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

PCSK9-deficient mice exhibit impaired glucose tolerance and pancreatic islet abnormalities

(2009) Majambu Mbikay et al.   FEBS LETTERS

LXR Regulates Cholesterol Uptake Through Idol-Dependent Ubiquitination of the LDL Receptor

(2009) Noam Zelcer et al.   SCIENCE

Inflammation stimulates the expression of PCSK9

(2008) Kenneth R. Feingold et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

PCSK9 is required for the disposal of non-acetylated intermediates of the nascent membrane protein BACE1

(2008) Mary Cabell Jonas et al.   EMBO REPORTS