Publication Highlights the Therapeutic Potential of BET Inhibition across Multiple Human Diseases
CALGARY, Alberta, Sept. 15, 2020 (GLOBE NEWSWIRE) -- Resverlogix Corp. ("Resverlogix" or the "Company") (TSX:RVX) announced today the recent publication of an article titled: “Inhibitors of bromodomain and extra terminal proteins for treating multiple human diseases”, in the peer-reviewed Medicinal Research Reviews.
The publication can be viewed using the following LINK.
“We assessed the current understanding of transcriptional mechanisms of BET inhibition to explain why BD2 selective compounds, like apabetalone, are showing a unique clinical response with fewer adverse events, making it appropriate for the treatment of chronic disease states including those explored in our development program,” said Dr. Ewelina Kulikowski, Senior Vice President, Research & Development at Resverlogix, and an author of the review. “Furthermore, this review – highlighting our leadership position in this research space – addresses the mechanisms by which apabetalone and other BET inhibitors can improve the maladaptive gene expression that underlies numerous human diseases.”
Publication Highlights include:
- A review of the role BET proteins play in enhancer and super-enhancer formation, and how that may drive multiple disease states
- A discussion of approaches to targeting BET proteins and the importance of bromodomain-selective binding among these compounds
- An overview of research into BET inhibitors, such as apabetalone, as therapeutics for chronic disease, including: cardiovascular, autoimmune, and metabolic diseases
- Emerging evidence for the improved safety and tolerability of BD2 selective compounds, including from the largest BETi trial to date, BETonMACE
Publication Background and Conclusions:
BET inhibitors represent a new paradigm in drug development due to their novel mechanism of action with potential to treat a broad spectrum of human diseases. This review details how targeted BET inhibitors do not simply reduce expression of every gene with BET-dependent transcription, but rather these therapeutic compounds act in concert with transcriptional machinery to target those genes that are upregulated or overexpressed by disease. The authors conclude that the research into selective BET inhibitors shows significant promise, writing: “Focused development of BD selective compounds is certain to alter and expand the clinical landscape for years to come.”
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 US 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.
Resverlogix common shares trade on the Toronto Stock Exchange (TSX:RVX).
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This news release may contain certain forward-looking information as defined under applicable Canadian securities legislation, that are not based on historical fact, including without limitation statements containing the words "believes", "anticipates", "plans", "intends", "will", "should", "expects", "continue", "estimate", "forecasts" and other similar expressions. In particular, this news release includes forward looking information related to the potential role of apabetalone in the treatment of 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. Our actual results, events or developments could be materially different from those expressed or implied by these forward-looking statements. We can give no assurance that any of the events or expectations will occur or be realized. By their nature, forward-looking statements are subject to numerous assumptions and risk factors including those discussed in our Annual Information Form and most recent MD&A which are incorporated herein by reference and are available through SEDAR at www.sedar.com. The forward-looking statements contained in this news release are expressly qualified by this cautionary statement and are made as of the date hereof. The Company disclaims any intention and has no obligation or responsibility, except as required by law, to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise.