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Message: BET inhibitors and Pulmonary Hypertension

Aureus over on IV posted on a new publication showing the benefits of the pan-BET inhibitor I-BET151 (from GSK) on pulmonary hypertension and COPD.

Inhibition of BET Proteins Reduces Right Ventricle Hypertrophy and Pulmonary Hypertension Resulting from Combined Hypoxia and Pulmonary Inflammation


Recall, Resverlogix has been exploring the benefits of apabetalone on pulmonary arterial hypertension (PAH) in pre-clinical studies and previously conveyed that 1) the effect of apabetalone on cells and in an animal model of PAH was positive' 2) three universities were collaborating on this work and working on paper now; and 3) there is even discussion about funding for that trial. I think these statements were made at last December's AGM.

Importantly, pan-BET inhibitors have major side effects and do not seem appropriate for long-term use. In the I-BET151 study cited above, they only dosed for 7 days in rats. Apabetalone is not a pan-BET inhibitor but is a bromodomain-2 selective BET inhibitor. Apabetalone has been shown to be safe for long-term use and some patients have been dosed for over 30 months so far. So a BD2-selective inhibitor like apabetalone would be more amenable to chronic use.

Cardiovascular diseases, renal function/chronic kidney disease, HIV latency, pulmonary hypertension, cognitive function (including Alzheimer's disease), Fabry disease, complement diseases (i.e. Paroxysmal Nocturnal Hemoglobinuria), inflammatory diseases, autoimmune diseases, neuroinflammation, muscular dystrophy/Facio Scapulo Humeral Dystrophy and many others not mentioned here.....such a long list of diseases that may benefit from apabetalone and/or other BET inhibitors. 



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