MOA apabetalone (rvx-208)This is nothng new but I came across a 2012 article from 2012 which illustrates Resverlogix understanding back at that time, then I added in the current understanding of the MOA. It illustrates the incredible progress mad by RVX over the past 5 years.
Old article from Investor’s Hub – 10/12/2012 https://investorshub.advfn.com/Resverlogix-Corp-RVXCF-25715/ APOA-I, HDL AND REVERSE CHOLESTEROL TRANSPORT
APOA-I AND HDL
The most abundant protein in HDL is ApoA-I and it serves as the building block for high-density lipoprotein (HDL or the "good cholesterol") particles. Increased production of ApoA-I protein will result in the synthesis of new HDL particles. These newly synthesized HDL particles are more' functional' because of their ample capacity to remove cholesterol from atherosclerotic plaques. The efflux of cholesterol from the plaque to HDL is called reverse cholesterol transport (RCT). The goal of enhanced RCT with newly synthesized HDL is to remove cholesterol from plaque in the arteries, subsequently regressing atherosclerosis. ApoA-I production therapeutics are the only technologies to date to efficiently remove and regress atherosclerotic plaque in high risk CVD patients.
REVERSE CHOLESTEROL TRANSPORT
Reverse cholesterol transport (RCT) is the natural process within the body that describes how HDL removes cholesterol from atherosclerotic plaques found in the wall of arteries. Cholesterol removed from the plaque is transported on the HDL particle to the liver for excretion from the body in the bile. Newly synthesized HDL particles are flat and empty and thus have the most function in mediating RCT.
RVX-208 & MOA
RVX-208
RVX-208 is a first-in-class, small molecule that inhibits BET bromodomains. It is currently being evaluated in a phase 2b clinical trial for its ability to reverse and/or stabilize atherosclerotic disease. RVX-208 acts to increase the production of ApoA-I protein which in turn is used to make new high-density lipoprotein (HDL) particles. These functional HDL particles are flat and empty and can efficiently remove plaque via reverse cholesterol transport (RCT), the natural process through which atherosclerotic plaque is transported out of the arteries and removed from the body by the liver.
Update to 2017
Current Understanding the MOA of apabetalone (rvx-208) Apabetalone impacts on the complement cascade(positive impact on the Immune system), reduction in coagulation, reduction in mediators that promote calcium deposition in the vasculature, reductions in mediators that promote inflammation of the vasculature, increased ApoA-I – positive effects on lipid content of HDL, reduced oral glucose absorption & endogenous production.