CALGARY, Alberta, June 08, 2022 (GLOBE NEWSWIRE) -- Resverlogix Corp. ("Resverlogix") (TSX:RVX) today announced the publication of an article entitled “Breaking boundaries: Pan BETi disrupt 3D chromatin structure, BD2-selective BETi are strictly epigenetic transcriptional regulators” in the journal Biomedicine & Pharmacotherapy. The article uncovers a clear mechanism for the improved safety, and reduced off-target effects, seen with BD2-selective BET inhibitors in comparison with non-selective BET inhibitors.
The article is published online HERE.
“This research helps us better understand the important differences between selective and non-selective BET inhibition as therapeutic strategies,” said Dr. Ewelina Kulikowski, Senior Vice President, Research & Development, and the senior author of the article. “BD2-selective inhibitors, such as apabetalone, can inhibit the expression of disease-causing genes without disrupting the fundamental functions of cells.”
Publication Highlights Include:
- A new role for BET protein BRD4 was discovered, in maintaining the higher order structure of chromatin at topologically associating domain (TAD) boundaries
- Maintaining the structure of TAD boundaries is critical for the basic functioning of cells, and disrupting the boundaries can lead to cell death
- As a result of differing interactions with BRD4, non-selective BET inhibitors disrupt TAD boundaries, while BD2-selective BET inhibitors do not
- These findings contribute to a potential mechanism underlying the differences in clinical safety outcomes observed between BD2-selective and non-selective BET inhibitors
Other Recent Publications
Another article, entitled “Inhibition of epigenetic reader proteins by apabetalone counters inflammation in activated innate immune cells from Fabry disease patients receiving enzyme replacement therapy”, was recently published in the journal Pharmacology Research & Perspectives. The article details the beneficial impacts of apabetalone treatment on inflammatory pathways in immune cells from Fabry disease patients. These findings suggest that apabetalone is a promising therapeutic candidate for the rare disorder. The article is available online HERE.
Apabetalone (RVX-208), is a first-in-class, small molecule, therapeutic candidate with an epigenetic mechanism of action. It is a BD2 (bromodomain) selective BET (bromodomain and extra-terminal) inhibitor that works in preventing and treating disease progression by regulating the expression of disease-causing genes.
Due to the extensive role for BET proteins in the human body, apabetalone, can simultaneously target multiple disease-related biological processes while maintaining a well-described safety profile – leading to a new way to treat chronic disease. Apabetalone received Breakthrough Therapy Designation from the US Food and Drug Administration (FDA) and is the only drug of its class with an established safety record in human clinical trials, with well over 4200 patient-years of safety data across 10 clinical trials.
Studies – published in prestigious scientific journals (including Cell) – demonstrate that apabetalone has the potential to act against COVID-19 with a unique dual-mechanism: first by preventing viruses from entering the cells and replicating; and second by averting excessive inflammatory reactions that can cause severe and lasting organ damage. The investigational treatment could potentially reduce the severity and duration of COVID-19. Apabetalone’s unique dual-mechanism also means that it has the potential to show efficacy against new COVID-19 variants and may even help fight other viruses.
Resverlogix has partnered with EVERSANA™, the pioneer of next generation commercial services to the global life sciences industry, to support the rapid commercialization of apabetalone for COVID-19 in Canada and the United States. EVERSANA™ is currently leading clinical outreach and advocacy for apabetalone in the Canadian market.
Apabetalone is the first therapy of its kind to receive Breakthrough Therapy Designation from the US Food and Drug Administration (FDA) – for a major cardiovascular indication – following the ground-breaking findings from the BETonMACE Phase 3 study. Data from BETonMACE showed apabetalone can potentially prevent major adverse cardiac events among high-risk cardiovascular disease patients who also have type 2 diabetes mellitus.
Founded in 2001, Resverlogix is a Calgary based late-stage biotechnology company and the world leader in epigenetics, or gene regulation, with the goal of developing first-in-class therapies for the benefit of patients with chronic disease.
Resverlogix is developing a new class of epigenetic therapies designed to regulate the expression of disease-causing genes. We aim to improve patients’ lives by restoring biological functions – altered by serious illnesses such as cardiovascular disease – back to a healthier state.
The Company’s clinical program is focused on evaluating the lead epigenetic candidate apabetalone for the treatment of cardiovascular disease and associated comorbidities, and COVID-19.
Resverlogix common shares trade on the Toronto Stock Exchange (TSX:RVX).
Follow us: Twitter: @Resverlogix_RVX. LinkedIn: https://www.linkedin.com/company/resverlogix-corp-/
Forward Looking Statements:
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 COVID-19, cardiovascular disease and associated comorbidities and other chronic 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.
For further information please contact: