18F-THK523: A novel in vivo tau imaging ligand for Alzheimer's disease

Michelle T. Fodero-Tavoletti, Nobuyuki Okamura, Shozo Furumoto, Rachel S. Mulligan, Andrea R. Connor, Catriona A. McLean, Diana Cao, Angela Rigopoulos, Glenn A. Cartwright, Graeme O'Keefe, Sylvia Gong, Paul A. Adlard, Kevin J. Barnham, Christopher C. Rowe, Colin L. Masters, Yukitsuka Kudo, Roberto Cappai, Kazuhiko Yanai, Victor L. Villemagne

Research output: Contribution to journalArticlepeer-review

284 Citations (Scopus)


While considerable effort has focused on developing positron emission tomography β-amyloid imaging radiotracers for the early diagnosis of Alzheimer's disease, no radiotracer is available for the non-invasive quantification of tau. In this study, we detail the characterization of 18F-THK523 as a novel tau imaging radiotracer. In vitro binding studies demonstrated that 18F-THK523 binds with higher affinity to a greater number of binding sites on recombinant tau (K18Δ280K) compared with β-amyloid1-42 fibrils. Autoradiographic and histofluorescence analysis of human hippocampal serial sections with Alzheimer's disease exhibited positive THK523 binding that co-localized with immunoreactive tau pathology, but failed to highlight β-amyloid plaques. Micro-positron emission tomography analysis demonstrated significantly higher retention of 18F-THK523 (48; P<0.007) in tau transgenic mice brains compared with their wild-type littermates or APP/PS1 mice. The preclinical examination of THK523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo, indicating that 18F-THK523 fulfils ligand criteria for human imaging trials.

Original languageEnglish
Pages (from-to)1089-1100
Number of pages12
Issue number4
Publication statusPublished - 2011 Apr


  • Alzheimer's disease
  • PET
  • dementia
  • imaging
  • tau


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