Norman Wong is on the schedule for the Alberta Epigenetics Network Summit to presents tomorrow morning, 3/22, on behalf of Resverlogix. Probably nothing new, but still exposure and networking. And a reminder that Richmond Club is on the schedule for Wednesday 3/23.

08. Apabetalone (RVX-208) the first selective bromodomain extra-terminal (BET) protein inhibitor in clinical development for treatment of cardiovascular disease (CVD).

Norman CW Wong, Ewelina Kulikowski, Jan Johansson, Mike Sweeney,

Resverlogix Corporation Calgary, AB, Canada,

Apabetalone (RVX-208) is an orally active small molecule that was discovered in Alberta. It is the first BET inhibitor to enter into human trials for treating CVD. RVX-208 selectively inhibits the second binding domain of BET proteins from complexing with its natural ligand acetylated lysine marks on the tail of histones. In so doing, RVX-208 modulates gene transcription and has effects on pathways known to play important roles in CVD risks including the complement, coagulation, inflammation, and metabolism as well as increasing levels of the apolipoprotein A-I (apoAI), the major protein in high density lipoprotein(HDL). In addition to preclinical studies in vitro and in vivo, RVX-208 has been tested in many human trials lasting up to 6 months that in total enrolled almost 1000 patients.

In post-hoc analysis of the most recent studies, patients with CVD receiving 200 mg/day of RVX-208 had a 55% relative risk reduction in major adverse cardiac events (MACE) compared to placebo. The multiple actions of apabetalone arising from our in vitro and in human trials are based on targeted inhibition of BET proteins.

We believe activity RVX-208’s activity in vitro and in vivo may underpin its ability to lower MACE by beneficially affecting several important pathways known to contribute CVD risks in addition to raising apoA-I/HDL. Apabetalone is currently in a phase 3 clinical trial.