Latest publication confirms BET inhibitors reduce the levels of critical receptors used by SARS-CoV-2 (COVID-19) to gain entry into cells, thereby reducing viral infection
CALGARY, Alberta, Dec. 22, 2020 (GLOBE NEWSWIRE) -- Resverlogix Corp. (“Resverlogix” or the “Company”) (TSX:RVX) is pleased to announce recent published findings in the high-impact journal, Proceedings of the National Academy of Sciences (PNAS), that further supports other 2020 publications and provides new evidence for the therapeutic potential of BET inhibitors in the treatment of COVID-19. A publication titled: “Targeting transcriptional regulation of SARS-CoV-2 entry factors ACE2 and TMPRSS2”, highlights the important role that host cell receptors play in enabling viral entry into cells, and presents direct evidence that BET inhibitors reduce SARS-CoV-2 (the scientific name for the virus responsible for COVID-19) infection by inhibiting the expression of these receptors. The publication also acknowledges Resverlogix and the Company’s plans to confirm the hypothesis with a clinical trial utilizing its advanced BET inhibition technology.
The publication can be viewed using the following LINK.
The findings are consistent with recent in-house studies performed by Resverlogix which demonstrated that apabetalone inhibits the expression of angiotensin-converting enzyme 2 (ACE2), the receptor utilized by the novel coronavirus to enter human cells. Further, preliminary data from collaborators – working with live coronavirus in multiple cell models – suggest apabetalone treatment prior to SARS-CoV-2 (COVID)-19) exposure significantly reduces viral infection.
“The PNAS study gives us the clearest evidence to date of the mechanism behind the efficacy of BET inhibitors in the treatment of COVID-19,” said Donald McCaffrey, President and CEO of Resverlogix. “So far, Resverlogix has been collaborating with three separate research groups each studying apabetalone in a live virus setting. We have reviewed the early data from these groups and have made the corporate decision to proceed with a human clinical trial as soon as possible. Our live virus data will be published upon completion of the work. We will be initiating our clinical design and applications prior to publication.
“As the only BET inhibitor with a well described clinical safety record, apabetalone is uniquely positioned as a potential therapeutic for this and future coronaviruses.”
Publication Highlights and Discussions Include:
- SARS-CoV-2 (COVID-19) enters cells in the lungs through the ACE2 receptor and is activated by another protein, transmembrane serine protease 2 (TMPRSS2)
- In mice, treatment with BET inhibitors was found to reduce levels of both ACE2 and TMPRSS2 in the lungs
- Data from human lung and prostate cells were also presented showing lowered expression of ACE2 and TMPRSS2, as well as decreased SARS-CoV-2 (COVID-19) infectivity with BET inhibition
- The study concludes that by both preventing viral entry and lessening inflammation, BET inhibitors could potentially treat both SARS-CoV-2 (COVID-19) infection and associated cytokine storms
- The authors highlight that Resverlogix has announced plans for a phase 2 COVID-19 clinical trial
As previously announced, an article published on March 23, 2020 revealed the interaction between SARS-CoV-2 (COVID-19) protein E with BET proteins. Following this finding, Resverlogix put out a call for collaborations, resulting in multiple partnerships, and in parallel initiated in-house preclinical research to further characterize and investigate apabetalone’s efficacy in treating COVID-19 infection.
Apabetalone is an investigational, phase 3 clinical candidate with safety data in more than 4,000 subjects. Additional details from the multiple, ongoing studies are expected to be presented in the coming few months.
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 timing and expectation of conducting a human COVID-19 clinical trial, the publishing of the data upon completion of the work, apabetalone as a potential therapeutic for COVID-19 and future coronaviruses and 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.