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Open AccessReview

Insight into the Development of PET Radiopharmaceuticals for Oncology

1
Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA
2
Department of Nuclear Medicine and Radiobiology, University of Sherbrooke, Sherbrooke, QC J1H 5N4, Canada
3
Department of Molecular Oncology, BC Cancer, Vancouver, BC V5Z 1L3, Canada
*
Author to whom correspondence should be addressed.
Cancers 2020, 12(5), 1312; https://doi.org/10.3390/cancers12051312
Received: 28 April 2020 / Revised: 17 May 2020 / Accepted: 18 May 2020 / Published: 21 May 2020
(This article belongs to the Special Issue Cancer Molecular Imaging)
While the development of positron emission tomography (PET) radiopharmaceuticals closely follows that of traditional drug development, there are several key considerations in the chemical and radiochemical synthesis, preclinical assessment, and clinical translation of PET radiotracers. As such, we outline the fundamentals of radiotracer design, with respect to the selection of an appropriate pharmacophore. These concepts will be reinforced by exemplary cases of PET radiotracer development, both with respect to their preclinical and clinical evaluation. We also provide a guideline for the proper selection of a radionuclide and the appropriate labeling strategy to access a tracer with optimal imaging qualities. Finally, we summarize the methodology of their evaluation in in vitro and animal models and the road to clinical translation. This review is intended to be a primer for newcomers to the field and give insight into the workflow of developing radiopharmaceuticals. View Full-Text
Keywords: positron emission tomography; diagnostic imaging; radiopharmaceuticals; radiochemistry; personalized medicine positron emission tomography; diagnostic imaging; radiopharmaceuticals; radiochemistry; personalized medicine
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MDPI and ACS Style

Lau, J.; Rousseau, E.; Kwon, D.; Lin, K.-S.; Bénard, F.; Chen, X. Insight into the Development of PET Radiopharmaceuticals for Oncology. Cancers 2020, 12, 1312.

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