
Resverlogix clinical candidate apabetalone featured as potential COVID-19 treatment in publication
On Mar. 23, 2020, Resverlogix announced a bioRxiv publication that has shown apabetalone to inhibit specialized proteins – called bromodomain and extraterminal domain (BET) proteins – from interacting with a SARS-CoV-2 viral protein, with potential for limiting viral reproduction in human cells.
The article titled: “A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing” by Gordon et. a.l, identified BRD2/4 as a binding partner of viral protein E. Apabetalone was shown to disrupt this interaction.
Resverlogix is developing apabetalone (RVX-208), a first-in-class, small molecule that is a selective BET (bromodomain and extra-terminal) inhibitor. Apabetalone is the first therapy of its kind to have been granted U.S. Food and Drug Administration (FDA) Breakthrough Therapy Designation – for a major cardiovascular indication – to help facilitate a time-efficient drug development program including planned clinical trials and plans for expediting the manufacturing development strategy.
BET inhibition is an epigenetic mechanism that can regulate disease-causing genes. Apabetalone is a BET inhibitor selective for the second bromodomain (BD2) within the BET proteins. This selective inhibition of apabetalone on BD2 produces a specific set of biological effects with potentially important benefits for patients with high-risk cardiovascular disease, diabetes mellitus, chronic kidney disease, end-stage renal disease treated with hemodialysis, neurodegenerative disease, Fabry disease, peripheral artery disease and other orphan diseases, while maintaining a well described safety profile.
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Source: Resverlogix Corp.
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