Insight into the Development of PET Radiopharmaceuticals for Oncology

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 o...

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Published inCancers Vol. 12; no. 5; p. 1312
Main Authors Lau, Joseph, Rousseau, Etienne, Kwon, Daniel, Lin, Kuo-Shyan, Bénard, François, Chen, Xiaoyuan
Format Journal Article
LanguageEnglish
Published Switzerland MDPI 21.05.2020
Subjects
Review
radiopharmaceuticals
positron emission tomography
diagnostic imaging
radiochemistry
personalized medicine
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Summary: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.
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ISSN:2072-6694
2072-6694
DOI:10.3390/cancers12051312