PET imaging of 11C-labeled thiamine tetrahydrofurfuryl disulfide, vitamin B1 derivative: First-in-human study

Vitamine B1 thiamine is an essential component for glucose metabolism and energy production. The disulfide derivative, tetrahydrofurfuryl (TTFD), more absorbent compared to readily-available water-soluble salts since it does not require the rate-limiting transport system required absorption. However, detailed pharmacokinetics of TTFD under normal pathological conditions were clarified yet. Recently, 11C-labeled synthesized by our group, their investigated PET imaging in rats. In this study, clarify whole body [11C]TTFD human healthy volunteers, we performed first-in-human study with [11C]TTFD, along radiation dosimetry humans. Synthesis was improved clinical study. Dynamic whole-body images acquired on three young male subjects after intravenous injection [11C]TTFD. VOIs defined source organs measure time-course uptake as percentage injected dose number disintegrations each organ. Radiation calculated OLINDA/EXM. We succeeded developing synthetic method imaging, various tissues almost plateaued at 10 min injection, afterward gradually increased brain urinary bladder (urine). %Injected high liver, kidney, bladder, heart, spine, brain, spleen, pancreas, stomach, salivary glands, order. per gram tissue also pituitary. By dosimetry, effective 5.5 ?Sv/MBq (range 5.2–5.7). Novel enabled which a safe tracer profile comparable other common 11C-PET tracers. Pharmacokinetics pharmacological different nutritional states could be further future quantitative studies. Noninvasive vivo pathophysiology thiamine-related function may provide diagnostic evidence novel information about vitamin deficiency tissues.