RVX-208 was one of the first BETi described after the advent of JQ1 and I-BET762 This quinazoline derivative was initially described as a BD2-selective compound, recognising the C-terminal bromodomain of BRD2 and BRD3, inhibiting these proteins with an IC50 of approximately 500 nM.67 RVX-208 is currently under clinical evaluation for the treatment of atherosclerosis and other high-density lipoprotein-linked diseases68–71 by virtue of its ability to increase the levels of apolipoprotein A1 (ApoA1) and reduce vascular inflammation in manner dependent on its inhibition of BET proteins.72 The gene discussed is APOA1; the disease is atherosclerosis.