Kimberly et al.1 reported the beneficial effects of IV glyburide on the clinical outcome of brain edema. We developed the carbon-11 radiolabeled analogue of glyburide to study the body distribution of this compound using PET imaging (figure, A). In a healthy person, the brain distribution of 11C-glyburide matched the cerebral blood volume, suggesting negligible blood–brain barrier (BBB) penetration (figure, B and C). This clinical observation corroborates preclinical findings suggesting that local changes in BBB structure and function are required for targeted delivery and favorable effects of glyburide to the injured brain tissue while minimizing potential side effects to the healthy brain.2
Summed PET projection (A), brain PET (B), and PET-MRI fusion (C) images obtained in a 30-year-old healthy man after IV injection of 11C-glyburide (60 minutes repeated whole-body scans). 11C-glyburide brain distribution (VT-brain = 0.023 mL.cm−3) was estimated using the Logan graphical analysis and the metabolite-corrected arterial input function.
Study registration
EudraCT 2017-001703-69.
Study funding
Supported by the French National Research Agency (IsotoPK, ANR-16-CE17-0011-001).
Disclosure
The authors report no disclosures relevant to the manuscript. Go to Neurology.org/N for full disclosures.
Appendix Authors
Footnotes
Go to Neurology.org/N for full disclosures.
- © 2019 American Academy of Neurology
References
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