Abstract
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.
Highlights
Positron emission tomography (PET) is a noninvasive nuclear imaging modality that is used, amongst many indications, for diagnosis, staging, and treatment monitoring of cancer [1]
These molecules differ in composition, they generally share the following attributes as imaging agents [7]: High specificity: The minimization of off-target binding ensures that sites of uptake are truly representative of the molecular pathology and not of a physiological process
Radiolabeled amino acids (AAs) represent one of the larger classes of PET radiopharmaceuticals based on endogenous molecules
Summary
Positron emission tomography (PET) is a noninvasive nuclear imaging modality that is used, amongst many indications, for diagnosis, staging, and treatment monitoring of cancer [1]. PET imaging is performed by administering, usually intravenously, a positron-tagged radiopharmaceutical into a patient [2]. We briefly summarize essential guidelines by regulatory bodies for preclinical assay of diagnostic radiopharmaceuticals to be performed before clinical trials. We hope this will serve as a resource for the nuclear medicine community and help expedite the progression of radiopharmaceuticals into clinical trials to improve patient care
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
