Development and evaluation of [11C]DPA-813 and [18F]DPA-814: novel TSPO PET tracers insensitive to human single nucleotide polymorphism rs6971
We have developed two novel PET tracers that display indiscriminately high binding affinity to both common isoforms of human TSPO, show favourable metabolic stability and brain penetration in rats, and significantly higher uptake in the spinal cord of a neuroinflammatory rat model of multiple sclerosis. Going forward, first-in-human clinical validation will mark a critical juncture in the development of these tracers, which could offer substantial improvements over existing imaging tools for detecting neuroinflammation, irrespective of genetic variations.
Authors
- Robert C. Schuit (ORCID: https://orcid.org/0000-0002-4962-2367)
- Albert D. Windhorst (ORCID: https://orcid.org/0000-0002-1250-7656)
- Eryn L. Werry (ORCID: https://orcid.org/0000-0002-6224-1286)
- Esther Kooijman
- Michael Kassiou (ORCID: https://orcid.org/0000-0002-6655-0529)
- Greta Sohler (ORCID: https://orcid.org/0000-0002-3065-4983)
- Jonathan J. Danon (ORCID: https://orcid.org/0000-0001-6242-1941)
- Wissam Beaino (ORCID: https://orcid.org/0000-0003-2216-4439)
- Elijah Genetzakis (ORCID: https://orcid.org/0009-0009-4381-7268)
- Johan van den Hoek
- Rens J. Vellinga
- Grace A. Cumbers (ORCID: https://orcid.org/0009-0002-3723-9114)
- Edward D. Harvey-Latham
Institutions
- The University of Sydney (AU)
- Amsterdam Neuroscience (NL)
- Amsterdam University Medical Centers (NL)
- Vrije Universiteit Amsterdam (NL)
Publication Details
- Journal
- European Journal of Nuclear Medicine and Molecular Imaging
- Published
- 2025-02-05
- DOI
- https://doi.org/10.1007/s00259-025-07109-1
- Citations
- 1
- Primary Topic
- Medical Imaging Techniques and Applications
- Type
- article
- Field-Weighted Citation Impact
- 1.36
Funders
- Australian Government
- University of Sydney
- Medical Research Council
- National Health and Medical Research Council