Publications

As leaders in the field of epigenetics, we continue to contribute to the scientific understanding of this important therapeutic space by sharing our findings in peer reviewed publications in leading life science academic journals. We also share our data with the scientific community at global conferences in the form of posters and oral presentations. Highlighted below are some of our recent publications and key articles that continue to build upon the progress of science in this field.

PUBLICATIONS

2023 Translational Neuroscience
The BET inhibitor apabetalone decreases neuroendothelial proinflammatory activation in vitro and in a mouse model of systemic inflammation

2023 Biomedicines
Apabetalone, a Clinical-Stage, Selective BET Inhibitor, Opposes DUX4 Target Gene Expression in Primary Human FSHD Muscle Cells

2023 Biomedicines
Apabetalone Downregulates Fibrotic, Inflammatory and Calcific Processes in Renal Mesangial Cells and Patients with Renal Impairment

2023 International Immunopharmacology
Dual mechanism: Epigenetic inhibitor apabetalone reduces SARS-CoV-2 Delta and Omicron variant spike binding and attenuates SARS-CoV-2 RNA induced inflammation

2023 Atherosclerosis
Epigenetic BET reader inhibitor apabetalone (RVX-208) counters proinflammatory aortic gene expression in a diet induced obesity mouse model and in human endothelial cells

2022 American Journal of Preventive Cardiology
Reduction in the risk of major adverse cardiovascular events with the BET protein inhibitor apabetalone in patients with recent acute coronary syndrome, type 2 diabetes, and moderate to high likelihood of non-alcoholic fatty liver disease

2022 Biomedicine & Pharmacotherapy
Breaking boundaries: Pan BETi disrupt 3D chromatin structure, BD2-selective BETi are strictly epigenetic transcriptional regulators

2022 Pharmacology Research & Perspectives
Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy

2022 American Journal of Respiratory and Critical Care Medicine
BET Protein Inhibition for Pulmonary Arterial Hypertension: A Pilot Study

2021 Journal of Alzheimer's Disease
Cognitive Effects of the BET Protein Inhibitor Apabetalone: A Prespecified Montreal Cognitive Assessment Analysis Nested in the BETonMACE Randomized Controlled Trial

2021 Cardiovascular Diabetology
Relation of Insulin Treatment for Type 2 Diabetes to the Risk of Major Adverse Cardiovascular Events After Acute Coronary Syndrome: An Analysis of the BETonMACE Randomized Clinical Trial

2021 Clinical Journal of the American Society of Nephrology
Effect of Apabetalone on Cardiovascular Events in Diabetes, CKD, and Recent Acute Coronary Syndrome

2021 Biomedicines
Bromodomain and Extraterminal Protein Inhibitor, Apabetalone (RVX-208), Reduces ACE2 Expression and Attenuates SARS-Cov-2 Infection In Vitro

2021 Cell Journal
BET Inhibition Blocks Inflammation-Induced Cardiac Dysfunction and SARS-CoV-2 Infection

2021 Cardiovascular Diabetology
Apabetalone and hospitalization for heart failure in patients following an acute coronary syndrome: a prespecified analysis of the BETonMACE study

2020 Clinical Epigenetics
BET protein inhibitor apabetalone (RVX-208) suppresses pro-inflammatory hyper-activation of monocytes from patients with cardiovascular disease and type 2 diabetes

2020 Medicinal Research Reviews
Inhibitors of bromodomain and extra‐terminal proteins for treating multiple human diseases

2020 Cardiovascular Therapeutics
Epigenetic modulation by apabetalone counters cytokine driven acute phase response in vitro, in mice and in patients with cardiovascular disease

2020 The Journal of the American Medical Association
Effect of Apabetalone Added to Standard Therapy on Major Adverse Cardiovascular Events in Patients With Recent Acute Coronary Syndrome and Type 2 Diabetes

2020 Current Opinion in Nephrology and Hypertension
Pharmacologic epigenetic modulators of alkaline phosphatase in chronic kidney disease

2019 Atherosclerosis

Apabetalone lowers serum alkaline phosphatase and improves cardiovascular risk in patients with cardiovascular disease

2019 American Heart Journal

Effect of selective BET protein inhibitor apabetalone on cardiovascular outcomes in patients with acute coronary syndrome and diabetes: Rationale, design, and baseline characteristics of the BETonMACE trial

2019 Clinical Epigenetics
Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism.

2019 American Journal of Respiratory and Critical Care Medicine
Multicenter Preclinical Validation of BET Inhibition for the Treatment of Pulmonary Arterial Hypertension.

2018 Atherosclerosis
Apabetalone Downregulates Factors and Pathways Associated with Vascular Calcification.

2018 American Journal of Cardiovascular Drugs
The Effect of Bromodomain and Extra-Terminal Inhibitor Apabetalone on Attenuated Coronary Atherosclerotic Plaque: Insights from the ASSURE Trial.

2018 Kidney & Blood Pressure Research
Apabetalone Mediated Epigenetic Modulation is Associated with Favorable Kidney Function and Alkaline Phosphatase Profile in Patients with Chronic Kidney Disease.

2018 Kidney International Reports
Benefit of Apabetalone on Plasma Proteins in Renal Disease. Supplemental Materials Available Here.

2017 American Journal of Cardiovascular Drugs
Selective BET Protein Inhibition with Apabetalone and Cardiovascular Events: A Pooled Analysis of Trials in Patients with Coronary Artery Disease.

2017 Molecular Pharmacology
RVX-297, a BET Bromodomain Inhibitor, Has Therapeutic Effects in Preclinical Models of Acute Inflammation and Autoimmune Disease.

2017 Journal of Cardiovascular Translational Research
Downregulation of the Complement Cascade In Vitro, in Mice and in Patients with Cardiovascular Disease by the BET Protein Inhibitor Apabetalone (RVX-208).

2016 Atherosclerosis
RVX-208, a BET-inhibitor for Treating Atherosclerotic Cardiovascular Disease, Raises ApoA-I/HDL and Represses Pathways that Contribute to Cardiovascular Disease.

2016 Data in Brief
Data on Gene and Protein Expression Changes Induced by Apabetalone (RVX-208) in ex vivo Treated Human Whole Blood and Primary Hepatocytes.

2016 Metabolism
Effects of the BET-inhibitor, RVX-208 on the HDL Lipidome and Glucose Metabolism in Individuals with Prediabetes: A Randomized Controlled Trial.

2015 Expert Opinion on Investigational Drugs
An Evaluation of RVX-208 for the Treatment of Atherosclerosis.

2015 European Biopharmaceutical Review
New Direction.

2014 Atherosclerosis
A Novel BET Bromodomain Inhibitor, RVX-208, Shows Reduction of Atherosclerosis in Hyperlipidemic ApoE Deficient Mice.

2013 PLoS One
RVX-208, an Inducer of ApoA-I in Humans, is a BET Bromodomain Antagonist.

2012 Cardiovascular Drugs and Therapy
ApoA-I Induction as a Potential Cardioprotective Strategy: Rationale for the SUSTAIN and ASSURE Studies

2011 Journal of the American College of Cardiology
Efficacy and Safety of a Novel Oral Inducer of Apolipoprotein A-I Synthesis in Statin-Treated Patients With Stable Coronary Artery Disease

POSTERS

2023 American College of Cardiology (ACC) Scientific Session
Epigenetic Bet Reader Inhibitor Apabetalone (RVX-208) Counters Profibrotic and Contractile Activity of Cardiac Fibroblasts with Potential Benefit for Heart Failure

2022 Clinical Trials on Alzheimer's Disease (CTAD) Congress
The Bromodomain And Extraterminal Domain Protein Inhibitor Apabetalone Inhibits The Neurotoxic Kynurenine Pathway In Monocytes And Brain Endothelial Cells

2022 ACC.22 American College of Cardiology
The epigenetic bet-inhibitor apabetalone reduces cardiovascular events in patients with type 2 diabetes, acute coronary syndrome and an elevated angulo non-alcoholic fatty liver disease fibrosis score - exploratory analysis of the BETonMACE trial

2021 Clinical Trials on Alzheimer’s Disease (CTAD) Congress
BET-Inhibition by Apabetalone and Cognitive Effects: A Pre-Specified MoCA Analysis Nested in the BETonMACE Randomized Controlled Trial

2021 Clinical Trials on Alzheimer’s Disease (CTAD) Congress
The Epigenetic Modulator Apabetalone Decreases Neuroinflammation in Blood Brain Barrier Cell Models and LPS-Treated Mice

2021 ERA-EDTA Congress
Apabetalone Downregulates Fibrotic, Inflammatory and Calcific Processes in Renal Mesangial Cells Which May Contribute to Reduced Cardiac Events Observed in CKD Patients

2021 European Society of Cardiology (ESC) Congress
Bromodomain and extraterminal (BET) protein inhibitor, apabetalone, reduces ACE2 expression and attenuates SARS-CoV-2 infection in vitro

2021 European Society of Cardiology (ESC) Congress
Reduction in the Risk of MACE with Apabetalone in Patients with Recent Acute Coronary Syndrome and Diabetes According to NAFLD Fibrosis Score: Exploratory Analysis of the BETonMACE Trial

2021 FSHD Society International Research Congress (FSH IRC)
Apabetalone, a Clinical-stage Cardiovascular Disease Drug, Inhibits DUX4 Expression in FSHD Cells

2021 American Heart Association (AHA) Scientific Sessions
Epigenetic BET Reader Inhibitor Apabetalone (RVX-208) Counters Proinflammatory Aortic Gene Expression in a DIO Mouse Model

2021 American Society of Nephrology: Kidney Week
Apabetalone Downregulates Fibrotic, Inflammatory and Calcific Processes in Renal Mesangial Cells: Mechanism for Reduced Cardiac Events in CKD Patients

2021 American College of Cardiology (ACC) Scientific Session
Apabetalone (RVX-208) Reduces ACE2 Protein Abundance and Prevents SARS-CoV-2 Spike Protein Binding to Human Lung Cells, a MOA That Could Attenuate Viral Entry

2021 American College of Cardiology (ACC) Scientific Session
Epigenetic BET Reader Inhibitor Apabetalone (RVX-208) Counters Proinflammatory Aortic Gene Expression In a Diet-Induced Obesity Mouse Model

2021 Alzheimer's Association International Conference (AAIC)
Favorable Cognitive Effects of the BET Protein Inhibitor Apabetalone in Patients 70 and Older

2021 The American Association of Immunologists (AAI): Virtual Immunity
Inhibition of Epigenetic Reader BET Proteins by Apabetalone Counters Inflammation in Activated Innate Immune Cells from Fabry Disease Patients Receiving ERT

2020 Advances in Alzheimer’s and Parkinson’s Therapies – An AAT-AD/PDTM Focus Meeting
The Epigenetic Modulator Apabetalone Downregulates Brain Endothelial Activation and Monocyte Adhesion

2020 ERA-EDTA Congress
Effects of the BET-Inhibitor Apabetalone on Cardiovascular Events in Patients With Type 2 Diabetes Mellitus and Acute Coronary Syndrome, According to Presence or Absence of Chronic Kidney Disease. A BETonMACE Trial Report.

2020 American Heart Association (AHA) Scientific Sessions
Reduction in the Risk of Major Adverse Cardiovascular Events with Apabetalone, a BET Protein Inhibitor, in Patients with Recent Acute Coronary Syndrome and Type 2 Diabetes According to Insulin Treatment: Analysis of the BETonMACE Trial

2020 American Heart Association (AHA) Scientific Sessions
BET Protein Inhibitor Apabetalone Suppresses Inflammatory Hyperactivation of Monocytes from Patients with Cardiovascular Disease and Type 2 Diabetes

2020 American Heart Association (AHA) Scientific Sessions
Apabetalone (RVX-208) Reduces ACE2 Expression in Human Cell Culture Systems, Which Could Attenuate SARS-CoV-2 Viral Entry

2020 Clinical Trials on Alzheimer's Disease (CTAD) Digital
The Epigenetic BET Protein Inhibitor Apabetalone Counters Brain Endothelial Activation and Monocyte Adhesion

2020 American Society of Nephrology: Kidney Week
Apabetalone, an Inhibitor of BET Proteins, Downregulates Alkaline Phosphatase and
Improves Cardiovascular Risk

2020 American College of Cardiology Scientific Sessions together with the World Congress of Cardiology
The BET Protein Inhibitor Apabetalone Reduces Congestive Heart Failure Incidence in Patients with Acute Coronary Syndrome and Diabetes: Results from the BETonMACE Trial

2020 American College of Cardiology Scientific Sessions together with the World Congress of Cardiology
Epigenetic Reader Inhibitor Apabetalone (RVX-208) Counters Proinflammatory Hyperactivation of CD14+ Monocytes from Patients with Type 2 Diabetes and Cardiovascular Disease

2019 Clinical Trials on Alzheimer's Disease (CTAD) Congress
Epigenetic Modulator Apabetalone Inhibits Monocyte Adhesion To Brain Endothelial Cells By Downregulating Key Neuroinflammation Markers In Vitro And In Vivo

2019 AHA Scientific Sessions
ALP Levels Predict Adverse Cardiovascular Outcomes and Cognitive Impairment in High Risk Patients

2019 American Society of Nephrology: Kidney Week Apabetalone Downregulates Alkaline Phosphatase and Improves Cardiovascular Risk

2019 American Society of Nephrology: Kidney Week Association of Serum Alkaline Phosphatase with CKD and Cognitive Function in Patients with Diabetes and Acute Coronary Syndrome

2019 American Society of Nephrology: Kidney Week Apabetalone Lowers Serum Alkaline Phosphatase in CVD Patients With and Without CKD and Improves Cardiovascular Risk

2019 Neuroscience 2019 Apabetalone Epigenetically Inhibits Monocyte Adhesion to Brain Endothelial Cells by Downregulating Key Neuroinflammation Markers In Vitro and In Vivo

2019 European Association for the Study of Diabetes (EASD) Annual Meeting Apabetalone Modulates Th1 Responses in Diabetes and CVD Through Intrinsic and Extrinsic Mechanisms: in vitro and in human study

2019 European Society of Cardiology (ESC) Congress Apabetalone (RVX-208) Inhibits Key Drivers of Vascular Inflammation, Calcification,
and Plaque Vulnerability Through a BET-dependent Epigenetic Mechanism

2019 European Society of Cardiology (ESC) Congress BET-inhibition with Apabetalone in Post-ACS Patients with Diabetes: Design and Baseline Characteristics of the BETonMACE Trial

2019 Alzheimer's Association International Conference (AAIC) Effects of the Epigenetic BET-Inhibitor Small Molecule Apabetalone on Cognition in Patients with Diabetes and Cardiovascular Disease.

2019 56th European Renal Association - European Dialysis and Transplant Association (ERA-EDTA) Congress 2019 Apabetalone, a Selective Bromodomain and Extra-Terminal (BET) Inhibitor, Reduces Serum FGF23 in Cardiovascular Disease and Chronic Kidney Disease Patients.

2019 American Diabetes Association's 79th Scientific Sessions (ADA 2019) Apabetalone (RVX-208) Attenuates an Inflammatory Milieu that Enhances Adhesion of Monocytes to Endothelial Cells in Type 2 Diabetes Mellitus with Cardiovascular Diasease Patients.

2019 87th European Atherosclerosis Society (EAS) Congress Apabetalone (RVX-208) Attenuates Inflammatory Milieu Underlying Adhesion of Monocytes to Endothelial Cells in Type 2 Diabetes Mellitus with Cardiovascular Disease Patients. 

2019 Vascular Discovery: From Genes to Medicine
Hepatic Expression of C-Reactive Protein is Epigenetically Regulated by BET Proteins and Inhibited by Apabetalone (RVX-208) in Vitro and in CVD Patients.

2019 Vascular Discovery: From Genes to Medicine
Apabetalone (RVX-208) Inhibits Key Pro-Atherogenic Mediators and Pathways in Diabetes and Inflammatory Conditions; in Vitro and in Patients.

2019 14th​ International Conference on Alzheimer's and Parkinson's Diseases
Epigenetic Inhibitor Apabetalone Downregulates Brain Endothelial and Microglial Cell Activation that Contributes To Neurodegenerative Disease.

2019 American College of Cardiology’s Scientific Session
BET Protein Inhibition and Cognition: A Pre-Specified Substudy of the BETonMACE Phase 3 Trial Evaluating Apabetalone in Patients With Diabetes and Acute Coronary Syndrome.

2019 American College of Cardiology’s Scientific Session
Apabetalone, an Epigenetic BET Inhibitor in a Phase 3 Trial, Inhibits Vascular Inflammation and Cellular Adhesion Leading to Beneficial Outcomes in CVD Patients.

2018 AHA Scientific Sessions
Apabetalone (RVX-208) Suppresses Expression of Key Vascular Inflammation Markers in Monocytes, Endothelial Cells and LPS-Challenged Mouse Liver and Monocyte Adhesiveness to Activated Endothelial Cells.

2018 AHA Scientific Sessions
Cardiovascular Evaluation of the Selective Bet Inhibitor, Apabetalone, in ACS Patients With Diabetes: Baseline Characteristics of the BETonMACE CV Outcomes Study.

2018 American Society of Nephrology (ASN) Kidney Week
Apabetalone Downregulates Factors and Pathways Associated with Vascular Calcification.

2018 Clinical Trials on Alzheimer's Disease Conference (CTAD - Barcelona)
Apabetalone, a BET Bromodomain Inhibitor, Suppresses Inflammatory Mediators in Microglia and Vascular Endothelial Cells that Contribute to Neurodegenerative Disease.

2018 Clinical Trials on Alzheimer's Disease Conference (CTAD - Shanghai)
Effect of the BET Protein Inhibitor Apabetalone on Serum Markers of Potential Importance for Cognitive Decline in Cardiovascular Disease Patients.

2018 Alzheimer's Association International Conference (AAIC)
Apabetalone (An Epigenetic BET-Inhibitor Small Molecule): A Substudy Evaluating Effects on Cognition in Diabetes Patients with Cardiovascular Disease.

2018 European Renal Association European Dialysis and Transplant Association (ERA-EDTA) Congress
BETonMACE Chronic Kidney Disease Sub-Study: Effects of the Selective BET-Inhibitor Apabetalone on Kidney Function and MACE in Post-ACS Patients with Diabetes and Estimated Glomerular Filtration Rate Below 60. 

2018 European Renal Association European Dialysis and Transplant Association (ERA-EDTA) Congress
Inhibition of BET Proteins with Apabetalone Reduces Mediators of Vascular Calcification In Vitro and in CKD Patients. 

2017 American Diabetes Association Scientific Sessions
Apabetalone (RVX-208) Lowers Major Adverse Cardiovascular Events (MACE) in Diabetes Mellitus by Affecting Complement Pathway and Microbiome Activity. 

2017 European Renal Association – European Dialysis and Transplant Association (ERA-EDTA) Congress
Effects of Apabetalone (RVX-208) on Serum Albumin in Subjects with CVD, Diabetes and Chronic Kidney Disease; a Post-Hoc Analysis of the ASSURE and SUSTAIN Clinical Trials. 

2017 European Renal Association – European Dialysis and Transplant Association (ERA-EDTA) Congress
Apabetalone, A Bromodomain and Extraterminal Protein Inhibitor, Decreases Key Factors in Vascular Calcification in Vitro and in Clinical Trials. 

2017 International Conference on Alzheimer's & Parkinson's Diseases
Apabetalone, a BET Bromodomain Inhibitor, Suppresses Inflammatory Mediators in Microglia that Contribute to Neurodegenerative Disease.

2017 Atherosclerosis, Thrombosis & Vascular Biology Scientific Sessions
Apabetalone (RVX-208), a Selective CET Protein Inhibitor, Reduces Expression of Acute Phase Response Markers in Vitro and In Patients with Cardiovascular Disease and Chronic Kidney Disease.

2016 American Society of Nephrology Conference
Apabetalone Reduces Levels of Key Markers Involved in Vascular Calcification. 

2016 American Heart Association Scientific Sessions
Apabetalone (RVX-208) Reduces Expression of Acute Phase Response Markers in Vitro and in Patients with Cardiovascular Disease.

2016 European Society of Cardiology Congress
Modulation of the Complement Cascade in Cardiovascular Disease Patients by a Bromodomain and Extraterminal (BET) Protein Inhibitor. 

2016 Atherosclerosis, Thrombosis & Vascular Biology Scientific Sessions
Apabetalone (RVX-208) has Anti-Atherosclerotic, Anti-Thrombotic and Anti-Inflammatory Effects in Patients with Cardiovascular Disease. 

2015 American Heart Association Scientific Sessions
RVX-208, a Selective Bromodomain Extra-Terminal (BET) Protein Inhibitor, Acts on Several Pathways to Benefit Cardiovascular Risk. 

2015 American Society of Nephrology Conference
Alkaline Phosphatase Lowering by Selective BET Inhibition, a Novel Mechanism for MACE Reduction in High Risk CVD, Diabetes and CKD Patients; a Post-hoc Analysis of Phase 2b Studies with Apabetalone (RVX-208).

2015 American Society of Nephrology Conference
Apabetalone (RVX-208), a First-in-Class Epigenetic BET Inhibitor, has Effects on ALP and eGFR in Subjects with CVD and CKD; a Post-hoc Analysis of ASSERT, SUSTAIN and ASSURE Clinical Trials.