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Zenith's BET Inhibitor ZEN-3694 is Currently Being Evaluated in Multiple Oncology Clinical Trials

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Message: AACR 2018

One important clarification to make. Not all bromodomain-2 selective BET inhibitors are created equal. Different inhibitors can have different structures, bind to different regions of the bromodomain acetyl-lysine binding pocket, elicit different conformational shifts in the bromodomain, and have different affinities for BD2 vs. BD1.

I may have mislead readers on this Zenith page and on the Resverlogix page into thinking that just because Abbvie has a BD-2 selective BET inhibitor in cancer trial, that it would work similar to apabetalone for MACE reductions. Similarly, I may have mislead readers into thinking that apabetalone may have anti-cancer effects similar to the Abbvie compound. I do not know if this is true for the various reasons stated above.

Also recall that Resverlogix/Zenith have another published BD-2 selective compound (RVX-297) that is effective for acute inflammation and auto-immune disorders. While effective for inflammation/auto-immune endpoints, RVX-297 may or may not elicit the cardiovascular protection or anti-cancer effects of the apabetalone or the Abbvie compound, respectively. Time will tell. These companies know much more about their compounds than is in the public domain.

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