This has been claimed by some on the forum, generally without evidence or with very unconvincing evidence. I’m going to post two relevant papers that provide some evidence, and would like to invite more data from anyone who knows of any — especially in humans:

First is this study, which has been cited before but not the relevant table:

Second is this mouse study, in which “The anti-seizure potential of these compounds was determined by evaluating the electroconvulsive seizure threshold in normal and epileptic mice. Rapamycin and everolimus only poorly penetrated into the brain (brain:plasma ratio 0.0057 for rapamycin and 0.016 for everolimus)” — so limited entry for both, but 4x as high with everolimus as rapamycin.

5 Likes

Good information. If we combine this with the information David Sabatini conveyed in the recent video, about how you may need several sequential dosings of rapamycin to help penetrate the blood brain barrier, (and given the 28 hour half life for everolimus vs. ~65 hour half life of rapamycin), it seems we would want to have a rapid succession of everolimus doses. Perhaps once a day for three days, or perhaps twice a day (though I hesitate to take either in the evening as it has seriously impacted my sleep in the past when I’ve done this).

1 Like

Everolimus has superior evidence for treating a form of brain tumor called SEGA in TSC disease, which could mean there is better evidence for crossing the BBB.

In the absence of such direct comparisons, the more robust clinical trial experience with everolimus combined with regulatory approvals by the FDA and the European Medicines Agency provide the most compelling reason favoring everolimus over sirolimus to treat SEGA and other TSC disease manifestations at this time.

3 Likes