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Identification of positron emission tomography (PET) tracer candidates by prediction of the target-bound fraction in the brain
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmaceutical Biosciences.
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2014 (English)In: EJNMMI Research, ISSN 2191-219X, E-ISSN 2191-219X, Vol. 4, 1-8 p., 50Article in journal (Refereed) Published
Abstract [en]

Background: Development of tracers for imaging with positron emission tomography (PET) is often a time-consuming process associated with considerable attrition. In an effort to simplify this process, we herein propose a mechanistically integrated approach for the selection of tracer candidates based on in vitro measurements of ligand affinity (K-d), non-specific binding in brain tissue (V-u,V-brain), and target protein expression (B-max). Methods: A dataset of 35 functional and 12 non-functional central nervous system (CNS) PET tracers was compiled. Data was identified in literature for K-d and B-max, whereas a brain slice methodology was used to determine values for V-u,V-brain. A mathematical prediction model for the target-bound fraction of tracer in the brain (f(tb)) was derived and evaluated with respect to how well it predicts tracer functionality compared to traditional PET tracer candidate selection criteria. Results: The methodology correctly classified 31/35 functioning and 12/12 non-functioning tracers. This predictivity was superior to traditional classification criteria or combinations thereof. Conclusions: The presented CNS PET tracer identification approach is rapid and accurate and is expected to facilitate the development of novel PET tracers for the molecular imaging community.

Place, publisher, year, edition, pages
2014. Vol. 4, 1-8 p., 50
Keyword [en]
Positron emission tomography, Non-specific binding, Imaging, Receptor occupancy
National Category
Radiology, Nuclear Medicine and Medical Imaging
Identifiers
URN: urn:nbn:se:uu:diva-260170DOI: 10.1186/s13550-014-0050-6ISI: 000358050900001PubMedID: 26116114OAI: oai:DiVA.org:uu-260170DiVA: diva2:846522
Available from: 2015-08-17 Created: 2015-08-17 Last updated: 2017-12-04Bibliographically approved

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Fridén, Markus

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