Narmac,

I don't know of any publicly disclosed data that discusses the ability of RVX-208 to cross the blood brain barrier (BBB) in humans or animal models. The only data I know of that potentially addresses the brain activity of RVX-208 are the studies that measured changes in plasma amyloid beta 40 levels (AB-40) before and after RVX-208 treatment (for example in ASSERT). However, this is an indirect measure of altered brain AB-40 levels that assumes 1) plasma AB-40 changes are due to brain changes in AB-40 levels; and 2) that RVX-208 crossed the BBB to directly cause these changes as opposed to an indirect mechansim not involving brain penetrance of RVX-208. For example, RVX-208 may be causing increased apo-AI transcription/secretion from liver and these small newly-formed HDL molecules subsequently cross the BBB to elicit effect on AB-40.

Surely, Resverlogix knows the tissue distribution of RVX-208. Whether they have ever publicly disclosed this data is something I don't know. BET inhibitors based upon the diazepine scaffold have been published to cross the BBB in animal models. However, RVX-208 is of a different scaffold, so the tissue-distribution and ability to cross the BBB may be different. 

https://www.ncbi.nlm.nih.gov/pubmed/?term=27388964

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4121371/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4035449/

One trial with OTX-015 in Glioblastoma Multiforme (GBM) Patients (https://clinicaltrials.gov/ct2/show/NCT02296476) was terminated, but I haven't dug into the reason why.

That's all I've got.

BearDownAZ