apabetalone   Click here for help

GtoPdb Ligand ID: 7034

Synonyms: QC-216 | RVX 208 | RVX-000222 | RVX-208
PDB Ligand
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 [2], and to block inflammation-mediated cardiac injury and dysfunction that is caused by SARS-CoV-2 infection (in a study using human cardiac organoids) [6]. It has been respositioned for potential to provide a cardio-protective therapy that prevents COVID-19-mediated cardiac damage.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 3
Hydrogen bond donors 2
Rotatable bonds 6
Topological polar surface area 93.67
Molecular weight 370.15
XLogP 3.86
No. Lipinski's rules broken 0
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Canonical SMILES OCCOc1c(C)cc(cc1C)c1nc(=O)c2c([nH]1)cc(cc2OC)OC
Isomeric SMILES OCCOc1c(C)cc(cc1C)c1nc(=O)c2c([nH]1)cc(cc2OC)OC
InChI InChI=1S/C20H22N2O5/c1-11-7-13(8-12(2)18(11)27-6-5-23)19-21-15-9-14(25-3)10-16(26-4)17(15)20(24)22-19/h7-10,23H,5-6H2,1-4H3,(H,21,22,24)
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Summary of Clinical Use Click here for help
RVX 208 (under alternate research code RVX000222) reached Phase 2 clinical trial in patients with dyslipidemia and coronary artery disease [7]. 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 Click here for help
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 [4].
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) [5].
Clinical Trials
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