- Guide to PHARMACOLOGY
Synonyms: QC-216 | RVX 208 | RVX-000222 | RVX-208
Compound class: Synthetic organic
Comment: Apabetalone (RVX 208) is a derivative of the plant polyphenol resveratrol. RVX 208 is an investigational inhibitor of BET bromodomain containing proteins, with potential anti-atherosclerotic action for the treatment of cardiovascular disease (CVD) [3-4].
SARS-CoV-2 and CIVID-19: Apabetalone (RVX 208) has been reported to reduce ACE2 expression and hence SARS-CoV-2 infection in vitro , and to block inflammation-mediated cardiac injury and dysfunction that is caused by SARS-CoV-2 infection (in a study using human cardiac organoids) . It has been respositioned for potential to provide a cardio-protective therapy that prevents COVID-19-mediated cardiac damage.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Summary of Clinical Use|
|RVX 208 (under alternate research code RVX000222) reached Phase 2 clinical trial in patients with dyslipidemia and coronary artery disease . In response to the SARS-CoV-2 pandemic, this agent was repositioned for potential to affect the clinical disease course via modulating inflammatory modulators (e.g. IL-6, IL-8, TNF-α and C-reactive protein) in hospitalised COVID-19 patients.|
|Mechanism Of Action and Pharmacodynamic Effects|
|RVX 208 appears to have similar anti-atherogenic properties to resveratrol [1,7].
RVX 208 binds in particular to the second bromodomain (BD2) of BET family member BRD4, which regulates ApoA-I expression through an epigenetic mechanism .
A phase I trial has indicated that RVX 208 may also have the ability to destroy β-amyloid plaques indicative of Alzheimer's disease (AD) .
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT04894266||An Open-Label Study of Apabetalone in Covid Infection||Phase 2/Phase 3 Interventional||Resverlogix Corp|