Nature Reviews Nephrology and Pfizer Inc. discuss BET bromodomain inhibition and apabetalone as viable drug candidates
CALGARY, May 23, 2017 /CNW/ - Resverlogix Corp. ("Resverlogix" or the "Company") (TSX: RVX) today highlighted two additional works involving its lead drug, apabetalone, one recently published by third party academics and one in the form of a patent application by Pfizer Inc. (Pfizer). The publication, titled "Alkaline phosphatase: a novel treatment target for cardiovascular disease in CKD," is published in the prominent journal Nature Reviews Nephrology. This article describes the mechanisms that link Alkaline Phosphatase (ALP) to vascular calcification, inflammation, and cardiovascular disease. The Pfizer patent application was filed for the purpose of protecting their invention of using BET-family bromodomain inhibitors as a method of increasing frataxin in the treatment of patients with Friedreich's ataxia. Resverlogix' apabetalone, a BET bromodomain inhibitor, is specifically listed in Pfizer's patent. The patent describes the ataxia as a rare regressive inherited disease characterized by progressive damage to the nervous system and movement problems.
"We welcome the attention drawn to Resverlogix and apabetalone from significant industry groups such as Nature Reviews Nephrology and Pfizer. 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 now drawing expanded attention from the global academic and pharmaceutical communities," stated Donald McCaffrey, President and Chief Executive Officer.
Discussion on ALP and Cardiovascular Disease in Chronic Kidney Disease (CKD)
In the May, 2017 edition, Nature Reviews Nephrology published an article titled: "Alkaline phosphatase: a novel treatment target for cardiovascular disease in CKD," (Haarhaus et al. Nature Reviews Nephrology). In addition to the discussion of the ALP mechanism and links to disease, the authors also discuss "new drugs that target ALP, which have the potential to improve cardiovascular outcomes without inhibiting skeletal mineralization." The article dedicates a paragraph to RVX-208 (apabetalone) and cites four different publications involving RVX-208 (apabetalone).
Findings on Frataxin Expression and Friedreich's Ataxia
Recently, Pfizer applied for a patent titled: "Regulators of Frataxin" (WO 2017/037567 A1), their invention relates to the expression of frataxin by utilizing BET-bromodomain inhibitors. The purpose of the invention is for the potential treatment of a rare disease called Friedreich' ataxia (FA). RVX-208 (apabetalone) was listed as a potentially effective agent against this disease which is present in about 1 in 50,000 people. The ataxia of Friedreich's ataxia occurs from the degeneration of nerve tissue in the spinal cord. Symptoms usually begin between 5 to 15 years of age, leading to wheelchair requirements and can eventually lead to early death often related to cardiovascular disease.
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, dialysis, 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. Apabetalone is currently in a Phase 3 trial, BETonMACE, in high-risk CVD patients with type 2 DM and low high-density lipoprotein (HDL), and in a Phase 2a kidney dialysis trial designed to evaluate biomarker changes and safety parameters with apabetalone in up to 30 patients with end-stage renal disease treated with hemodialysis.
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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 relating to the potential role of apabetalone in the treatment of CVD, DM, chronic kidney disease, end-stage renal disease treated with hemodialysis, Alzheimer's disease, Alkaline phosphatase (ALP), vascular calcification, inflammation, Friedreich's ataxia, expression of frataxin, and 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.
SOURCE Resverlogix Corp.