Re: RVX 297 publication news from rndtbl from IV
in response to
by
posted on
Oct 03, 2017 11:54AM
Thanks Nextblockbuster (and rndtbl)! I added this publication to the link library. Very nice to see the studies on the preclinical models of acute inflammation and autoimmunity published. Interesting that both RVX-208 and RVX-297 are bromodomain-2 selective BET bromodomain inhibitors. However, this publication did not compare the two side by side. It makes me wonder....how RVX-208 would compare to RVX-297 for these models of acute inflammation and autoimmunity? And how would RVX-297 compare to RVX-208 for all of the endpoints that RVX-208 is known to modulate?
Perhaps some clues from a previous RVX-297 paper. The take-home message....not all bromodomain-2 selective BET inhibitors will elicit equal effects.
"RVX-297 is a 4-quinazolinone derivative related to RVX-208 with an alkylpyrrolidine side chain off the di-methyl substituted phenyl ring (Fig.1A). In spite of the structural similarity to RVX-208, RVX-297 has demonstrated a different pharmacodynamical profile, as well as distinct cellular and biological activity which was elucidated in the autoimmune disease models of multiple sclerosis and arthritis [14,15]." Note: References 14 and 15 are posters presented at conferences that are now published as part of the latest paper.
"The RVX-297 selectivity profile is somewhat similar to the BD2-preferential selectivity profile reported for RVX-208 [5,8] with RVX-297 being ~2 times more selective than RVX-208."