PET microdosing of CNS drugs

Purpose Positron emission tomography (PET) is an important tool in the discovery and development of drugs targeting the central nervous system. The current review purports to give a brief overview of methods used in the labeling and quantitative evaluation of brain disposition and kinetics of radiol...

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Bibliographic Details
Published in:Clinical and translational imaging : reviews in nuclear medicine and molecular imaging 2017-06, Vol.5 (3), p.291-298
Main Authors: Schou, Magnus, Varnäs, Katarina
Format: Article
Language:eng
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Summary:Purpose Positron emission tomography (PET) is an important tool in the discovery and development of drugs targeting the central nervous system. The current review purports to give a brief overview of methods used in the labeling and quantitative evaluation of brain disposition and kinetics of radiolabeled drug molecules. These radiolabeled drug molecules are typically administered in microgram amounts, hence the concept microdosing. Methods A survey of the literature (using Pubmed and Scopus) was performed to identify papers that comprised information on methods used for radiolabeling, preclinical and/or clinical PET evaluation of CNS drugs and/or drug candidates. Results A selection of 65 papers were identified following the literature review. In addition to including papers that illustrate the relevant methodologies used in PET microdosing, a few reports on the practical use of PET microdosing in a drug discovery and development setting were also included. Conclusion PET microdosing is increasingly used to support candidate drug selection in drug discovery and development. Although it is most commonly used in the development of central nervous system drugs, it has recently also been used for neuro-oncology purposes.
ISSN:2281-5872
2281-7565