"Due to the dramatic growth of BET Bromodomain publications over the past decade, it is not surprising that our advanced Phase 3 compound, apabetalone, is drawing expanded attention from the global academic community. Over the past decade BET Bromodomain publications have grown by over 2,700 percent. Resverlogix publications have increased even more dramatically during this same timeframe." stated Donald McCaffrey, President and Chief Executive Officer.
Findings on Retinal Degeneration
In January 2017, the Journal of Neuroinflammation published an article titled "Photoreceptor protection via blockade of BET epigenetic readers in a murine model of inherited retinal degeneration" (Zhao et al. Journal of Neuroinflammation (2017) 14:14) where BET inhibitors, including apabetalone (RVX-208), were tested in an animal model of retinal degeneration. The authors concluded that inhibition of the epigenetic readers rescued photoreceptor degeneration in the eye, likely via the suppression of microglial activation. Moreover, the findings demonstrated differential effects of BET inhibitors based on their bromodomain selectivity, which were suggested to have distinct functions in this pathogenic process. BET protein inhibition was identified as a potential novel therapeutic strategy to treat neurodegenerative disease states where microglial activation or pathogenic cell state transformation plays a role, with potential impact for diseases such as retinitis pigmentosa.
Findings on Facioscapulohumeral Muscular Dystrophy
FSHD is a debilitating disease that arises from a genetic defect and is one of the most common types of muscular dystrophy affecting approximately 12 in 100,000 people. This muscle disorder initially affects the muscles of the face, shoulder blades and upper arms with eventual spread to other muscles of the body.
In research conducted at Saint Louis University and subsequently used in a patent application, BET inhibitors were shown to inhibit expression of the DUX4 gene, which is expected to reduce the severity of symptoms in this disease. Apabetalone treatment, when compared to other BET inhibitors, demonstrated a similar repression of DUX4, however no transient suppression of MYH2 (a differentiation marker for myotubes) was observed. This differential effect on the marker of muscle cell differentiation was unique to apabetalone and demonstrated the distinct properties of this BET inhibitor.
Treatment of FSHD via BET protein inhibition offers a novel therapeutic indication for apabetalone and this class of compounds.
Resverlogix is developing apabetalone (RVX-208), a first-in-class, small molecule that is a selective BET (bromodomain and extra-terminal) inhibitor. BET bromodomain inhibition is an epigenetic mechanism that can regulate disease-causing genes. Apabetalone is the first and only BET inhibitor selective for the second bromodomain (BD2) within the BET protein called BRD4. This selective inhibition of apabetalone on BD2 produces a specific set of biological effects with potentially important benefits for patients with diseases such as high-risk cardiovascular disease (CVD), diabetes mellitus (DM), chronic kidney disease, Alzheimer's disease, Orphan diseases, and peripheral artery disease, while maintaining a well described safety profile. Apabetalone is the only selective BET bromodomain inhibitor in human clinical trials, currently in a Phase 3 trial BETonMACE in high-risk CVD patients with type 2 DM and low high-density lipoprotein (HDL).
Resverlogix common shares trade on the Toronto Stock Exchange (TSX: RVX).
For further information please visit www.resverlogix.com.
Follow us on Twitter: @Resverlogix_RVX (https://twitter.com/resverlogix_rvx), or on our blog at http://www.resverlogix.com/blog
For further information please contact:
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 relating to the potential role of apabetalone in the treatment of CVD, DM, chronic kidney disease, Alzheimer's disease, Facioscapulohumeral Muscular Dystrophy (FSHD), retinis pigmantosa, Orphan diseases, and peripheral artery disease. 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.
SOURCE Resverlogix Corp.