Physicians' Academy for Cardiovascular Education

BET Inhibition

BET bromodomain inhibition is an epigenetic mechanism that can modify gene transcription. BET inhibitors selective for BRD4-BD2 are currently tested in clinical trials with potentially important benefits for patients with diseases such as cardiovascular disease, diabetes mellitus, chronic kidney disease, peripheral artery disease.

First inhibitor of BET transcriptional regulators improves kidney function in CKD patients with CAD

Literature - Apr. 3, 2018 - Kulikowski E, et al. - Kidney Blood Press Res. 2018
Apabetalone Mediated Epigenetic Modulation is Associated with Favorable Kidney Function and Alkaline Phosphatase Profile in Patients with Chronic Kidney Disease

Meeting Impression | Managing Diabetes & CVD: Is epigenetics a new way forward?

August 26, 2017 - ESC

Summary | Insights from the first trials in epigenetics in human: What is the way forward?

August 26, 2017 - Prof. Stephen Nicholls (Adelaide, Australia)

Insights from the first trials in epigenetics in human: What is the way forward?

10' education - Oct. 20, 2017 - Barcelona, Spain - Stephen Nicholls, MD, Adelaide, Australia - PACE-CME symposium at ESC 2017

Promise of epigenetic modulation as a target in atherosclerotic patients

10' education - Aug. 26, 2017 - Barcelona, Spain - Erik SG Stroes, MD, Amsterdam, the Netherlands - PACE-CME symposium at ESC 2017

The Clinical Unmet need in the patient with Diabetes and ACS

10' education - Aug. 26, 2017 - Barcelona, Spain - Kausik Ray, MD Imperial College London United Kingdom - PACE-CME symposium held at ESC 2017

BET inhibition in renal and cardiovascular disease: What is the clinical roadmap?

10' education - June 5, 2017 - ERA-EDTA, Madrid Spain - Kamyar Kalantar-Zade, MD UC Irvine School of Medicine Irvine, Ca, USA

Molecular mechanisms involved in the beneficial effect of BET inhibition in experimental renal disease

10' education - June 5, 2017 - ERA-EDTA, Madrid Spain - Marta Ruiz-Ortega – Fundación Jiménez Díaz, Madrid, Spain

The high risk diabetes patient: What is the need for novel approaches to reduce cardiovascular and renal risk?

10' education - June 5, 2017 - ERA-EDTA, Madrid Spain - Luis M Ruilope, MD – Hospital 12 de Octubre, Madrid, Spain

Investigational epigenetic therapy lowers incidence of MACE in phase 2b study

3' education - Nov. 15, 2016 - AHA 2016, New Orleans, LA, USA - Dr. Norman Wong, Calgary, AB, Canada

Epigenetics: A closer look at BET inhibition

Sep. 5, 2016

Understanding BET inhibition as a novel pathway for cardiovascular risk modulation

10' education - Aug. 28, 2016 - ESC 2016, Rome - Jorge Plutzky, MD – Brigham and Women’s Hospital, Harvard Medical School, Boston, MA, USA - Recorded at PACE-CME symposium at ESC 2016

BET inhibition in cardiovascular disease: A new dawn?

10' education - Aug. 28, 2016 - ESC 2016, Rome - John Kastelein, MD – Academic Medical Center, Amsterdam, The Netherlands - Recorded at PACE-CME symposium at ESC 2016

The high risk diabetes patient with cardiovascular disease: What else can we target to reduce cardiovascular risk?

10' education - Aug. 28, 2016 - ESC 2016, Rome - Kausik Ray, MD – Imperial College London, United Kingdom - Recorded at PACE-CME symposium at ESC 2016

First inhibitor of BET transcriptional regulators improves kidney function in CKD patients with CAD

Literature - Apr. 3, 2018 - Kulikowski E, et al. - Kidney Blood Press Res. 2018
In 48 patients with chronic kidney disease and coronary artery disease, apabetalone had beneficial effects on alkaline phosphatase levels and estimated glomerular filtration rate.

In 48 patients with chronic kidney disease and coronary artery disease, apabetalone had beneficial effects on alkaline phosphatase levels and estimated glomerular filtration rate.

Meeting Impression | Managing Diabetes & CVD: Is epigenetics a new way forward?

August 26, 2017 - ESC
August 26, 2017 - ESC

In this educational program, which was held at the ESC Congress 2017 in Barcelona, Spain, epigenetic regulation of gene expression in patients at high CV risk with diabetes was reviewed

Summary | Insights from the first trials in epigenetics in human: What is the way forward?

August 26, 2017 - Prof. Stephen Nicholls (Adelaide, Australia)
August 26, 2017 - Prof. Stephen Nicholls (Adelaide, Australia)

Prof Nicholls shared some insights from the first human trials on epigenetic approaches to treat CVD. More specifically, he summarized the findings from the first trials with apabetalone.

Summary | Promise of epigenetic modulation as a target in atherosclerotic patients

August 26, 2017 - Prof. Erik Stroes (Amsterdam, The Netherlands)
August 26, 2017 - Prof. Erik Stroes (Amsterdam, The Netherlands)

Prof Stroes explained epigenetics and epigenetic modulation. Moreover, he summarized data from studies with apabetalone, a BET inhibitor, and the first trial results with apabetalone.

Insights from the first trials in epigenetics in human: What is the way forward?

10' education - Oct. 20, 2017 - Barcelona, Spain - Stephen Nicholls, MD, Adelaide, Australia - PACE-CME symposium at ESC 2017
Lecture by Prof Stephen Nicholls held at symposium on BET Inhibition: Managing high risk diabetes patient with cardiovascular disease: What works, and what else can we do?

This lecture was part of a CME accredited symposium: 'Managing Diabetes & CVD: Is epigenetics a new way forward?' held at ESC 2017 in Barcelona on August 26, 2017

BET inhibition may lower CV events in high risk CVD patients, suggests hypothesis-generating analysis

Literature - Oct. 18, 2017 - Nicholls SJ et al. - Am J Cardiovasc Drugs. 2017

Pooled analysis of phase II studies evaluating apabetalone suggest that this epigenetic therapeutic may yield clinical benefit for CVD patients with low HDL-C, diabetes, and elevated hsCRP levels.

Promise of epigenetic modulation as a target in atherosclerotic patients

10' education - Aug. 26, 2017 - Barcelona, Spain - Erik SG Stroes, MD, Amsterdam, the Netherlands - PACE-CME symposium at ESC 2017
Lecture by Prof Erik Stroes held at symposium on BET Inhibition: Managing high risk diabetes patient with cardiovascular disease: What works, and what else can we do?

This lecture was part of a CME accredited symposium: 'Managing Diabetes & CVD: Is epigenetics a new way forward?' held at ESC 2017 in Barcelona on August 26, 2017

The Clinical Unmet need in the patient with Diabetes and ACS

10' education - Aug. 26, 2017 - Barcelona, Spain - Kausik Ray, MD Imperial College London United Kingdom - PACE-CME symposium held at ESC 2017
Lecture by Prof Kausik Ray held at symposium on BET Inhibition: Managing high risk diabetes patient with cardiovascular disease: What works, and what else can we do?

This lecture was part of a CME accredited symposium: 'Managing Diabetes & CVD: Is epigenetics a new way forward?' held at ESC 2017 in Barcelona on August 26, 2017

BET inhibition in renal and cardiovascular disease: What is the clinical roadmap?

10' education - June 5, 2017 - ERA-EDTA, Madrid Spain - Kamyar Kalantar-Zade, MD UC Irvine School of Medicine Irvine, Ca, USA
Kamyar Kalantar-Zade, MD shows the data based on which alkaline phosphatase is emerging as a prognostic biomarker of CV events. BET inhibition with apabetalone lowers ALP, and may thus be a promising therapeutic strategy.

Kamyar Kalantar-Zade, MD shows the data based on which alkaline phosphatase is emerging as a prognostic biomarker of CV events. BET inhibition with apabetalone lowers ALP, and may thus be a promising therapeutic strategy.

Molecular mechanisms involved in the beneficial effect of BET inhibition in experimental renal disease

10' education - June 5, 2017 - ERA-EDTA, Madrid Spain - Marta Ruiz-Ortega – Fundación Jiménez Díaz, Madrid, Spain
Marta Ruiz-Ortega sheds light on the new and exciting field of epigenetics, and how BET inhibition might provide an interesting therapeutic target in renal disease. She shares experimental data dat demonstrate the beneficial effects of BET inhibition.

Marta Ruiz-Ortega sheds light on the new and exciting field of epigenetics, and how BET inhibition might provide an interesting therapeutic target in renal disease. She shares experimental data dat demonstrate the beneficial effects of BET inhibition.

The high risk diabetes patient: What is the need for novel approaches to reduce cardiovascular and renal risk?

10' education - June 5, 2017 - ERA-EDTA, Madrid Spain - Luis M Ruilope, MD – Hospital 12 de Octubre, Madrid, Spain
Luis M Ruilope, MD looks at the evidence showing that currently available therapies leave room for improvement in the reduction of CV events in patients with diabetes and chronic kidney disease.

Luis M Ruilope, MD looks at the evidence showing that currently available therapies leave room for improvement in the reduction of CV events in patients with diabetes and chronic kidney disease.

Investigational epigenetic therapy lowers incidence of MACE in phase 2b study

3' education - Nov. 15, 2016 - AHA 2016, New Orleans, LA, USA - Dr. Norman Wong, Calgary, AB, Canada
Epigenetic apabetalone or RVX-208 that alters chromatin structure and gene activity gave clinical benefit in phase 2 study.

AHA 2016 The orally active epigenetic drug RVX-208 or apabetalone that alters gene activity by modifying chromatin structure, lowered the incidence of MACE in a phase 2b study. This effect could not entirely be attributed to an effect on HDL, explains dr. Norman Wong.