On Jun. 1, 2020, Resverlogix announced that it is moving forward with a plan to further evaluate apabetalone’s impact on COVID-19 in both a preclinical and clinical setting. A first step will be to investigate whether apabetalone treatment of human cells susceptible to 2019 novel coronavirus (2019-nCoV) infection will impact the replication cycle of the virus. Initial work – undertaken in an approved Biological Safety Level 3 laboratory (BSL3) – commenced with additional work with other third-party laboratories expected. In parallel, cell factors critical to 2019-nCoV infection will be assessed in-house for apabetalone-mediated regulation.

An additional step will be to proceed with an open-label study to assess the safety and efficacy of a clinical course of oral apabetalone in hospitalized subjects with 2019-nCoV infection on top of standard of care compared to standard of care alone. Endpoints will include clinical progression, an evaluation of viral levels via nasal and pharyngeal swabs, as well as the effect of apabetalone on key virus-related biomarkers including ACE2 and others within the renin-angiotensin system, as well as an inflammatory panel of markers including IL6, IL8, CRP, etc. in hospitalized subjects with 2019-nCoV infection.

The safety of apabetalone has been demonstrated in >1900 subjects in completed Phase 1, Phase 2 and Phase 3 clinical studies, including >1700 patients with cardiovascular disease. Overall, apabetalone was generally well tolerated and serious adverse events were similar in placebo and active-treated subjects.

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.