2. Academic Validation
  3. 18F-THK523: a novel in vivo tau imaging ligand for Alzheimer's disease

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

  • Brain. 2011 Apr;134(Pt 4):1089-100. doi: 10.1093/brain/awr038.
Michelle T Fodero-Tavoletti 1,  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
Affiliations

Affiliation

  • 1 Department of Pathology, The University of Melbourne, Victoria, 3010, Australia.
PMID: 21436112 DOI: 10.1093/brain/awr038
Abstract

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 (18)F-THK523 as a novel tau imaging radiotracer. In vitro binding studies demonstrated that (18)F-THK523 binds with higher affinity to a greater number of binding sites on recombinant tau (K18Δ280K) compared with β-amyloid(1-42) 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 (18)F-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 (18)F-THK523 fulfils ligand criteria for human imaging trials.

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