Does Venetoclax Cross the Blood/Brain Barrier?

[DRM18]

Just curious. ... Look, I can Google as well as the next person, but I don’t always know how to interpret what I find. As is the case with my question here. Some sources I found say yes, some say “we dunno,” leaving me back where I started: knowledgeless. Help?

[Smith123456]

the answer is it's probably never been studied. The only way to know would be an autopsy where brain damage had been suspected. Venclexta hasn't been around enough to have this happen.

[cajunjeff]

Yes there is evidence venetoclax does cross the blood brain barrier.

ncbi.nlm.nih.gov/pmc/articl...

For the first time, we observed that the drug crossed the blood-brain barrier with a concentration close to the IC50 in CLL, and we report a potential efficacy of venetoclax combined with IT treatment in CLL with CNSi. In fact, a contribution of IT therapy to CNS disease clearance is likely, particularly in the early phase, where an additive effect of venetoclax can be hypothesized; moreover, the drug played a major role in the long-term response.

The blood-brain barrier penetration of venetoclax, together with its broad spectrum of action in hematologic malignancies, may lead the way to new treatment options in CNS localizations.

[DRM18 in reply to cajunjeff]

Thanks so much, oh wise & resourceful sir. That’s exactly what I was hoping to learn.