Journal of Biomolecular Screening | Year: 2013
It has now been almost 20 years since the discovery of p38 MAP kinase and its role in inflammatory cytokine synthesis through reverse pharmacology and its subsequent exploration as a potential target for autoimmune and other diseases. At the time of its discovery, the use of cell-based phenotypic screens to identify new molecular targets was at its infancy, and while p38 MAP kinase was not the first target to be identified this way, it provides a useful model for reviewing the pros and cons of this approach and the subsequent impact it can have on discovering new medicines. © 2013 Society for Laboratory Automation and Screening. Source
Resverlogix | Date: 2013-10-09
Compounds that are useful in the synthesis of 2-amino-4,6-dimethoxybenzamide derivatives and other benzamide compounds.
Resverlogix | Date: 2014-10-14
The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
Resverlogix | Date: 2012-10-31
The present disclosure relates to novel solid pharmaceutical formulations and process for their preparation. The present disclosure also provides, in part, methods of using the pharmaceutical formulations for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
News Article | October 26, 2015
Apabetalone will be evaluated in a Phase 3 clinical trial in high-risk coronary artery disease and type 2 diabetes mellitus patients Resverlogix Corp. (the "Corporation") (TSX:RVX) today announced the commencement of a Phase 3 clinical trial called 'BETonMACE' with lead drug apabetalone (RVX-208) in high-risk patients with coronary artery disease (CAD) and type 2 diabetes mellitus (DM). Resverlogix has received initial approval from the regulatory authority and ethics committee in the first three countries: Belgium, Hungary and Israel, which will represent approximately 15 investigative sites of an expected 175 site trial. The first site initiation visit was held today and with drug now available to the centers, enrollment of patients will commence. Over the course of the coming months, additional investigative sites will be activated. BETonMACE will assess the effect of apabetalone (RVX-208) on time to first occurrence of Major Adverse Cardiovascular Events (MACE) in high-risk type 2 DM patients with CAD. The Phase 3 trial will be double-blinded, randomized, parallel group, placebo-controlled, with up to 104 weeks of dosing. MACE is defined as cardiovascular death, non-fatal myocardial infarction (MI), hospitalization for cardiovascular disease events or stroke. All subjects will remain on a high-dose statin therapy (atorvastatin or rosuvastatin), with the experimental group receiving 200 mg/day of apabetalone in the form of 100 mg capsules twice daily. Primary outcome measures will be time to first occurrence of MACE as defined above. Secondary outcome measures and additional trial details and updates can be found at: http://www.clinicaltrials.gov and/or http://www.clinicaltrialsregister.eu/. 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. Resverlogix's Phase 3 clinical trial BETonMACE in high-risk CVD patients with type 2 DM and low high-density lipoprotein (HDL) has now commenced. Resverlogix's common shares trade on the Toronto Stock Exchange (TSX: RVX). For further information please visit http://www.resverlogix.com. We can be followed on our blog at http://www.resverlogix.com/blog and via Twitter @Resverlogix_RVX https://twitter.com/resverlogix_rvx. 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 Company's Phase 3 clinical trial and the potential role of apabetalone in the treatment of CVD, DM, chronic kidney disease, Alzheimer's disease, 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 http://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: