apabetalone

Apabetalone is an orally available small molecule drug developed by Resverlogix. It is a selective inhibitor of bromodomain and extra-terminal domain (BET) proteins, particularly targeting the second bromodomain (BD2) of bromodomain-containing protein 4 (BRD4). By inhibiting BET proteins, apabetalone modulates gene expression through epigenetic mechanisms—specifically reducing transcription of genes involved in inflammation and vascular calcification. This leads to increased ApoA-I gene expression and higher levels of high-density lipoprotein (HDL), promoting reverse cholesterol transport and potentially stabilizing atherosclerotic plaques. Apabetalone also exhibits anti-inflammatory effects by downregulating pro-inflammatory mediators in various cell types relevant to cardiovascular disease (CVD). Clinical trials have evaluated its efficacy for reducing major adverse cardiovascular events in patients with type 2 diabetes, low HDL cholesterol, or elevated inflammatory markers. Additionally, preclinical studies suggest potential benefits in chronic kidney disease by reducing fibrosis and extracellular matrix production as well as possible antiviral activity against SARS-CoV-2 via downregulation of ACE2 and CD26 receptors[1][5][6][8].

Other names

2-(4-(2-Hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one1044870-39-4