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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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.
AbstractList 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.
Author Lau, Joseph
Rousseau, Etienne
Lin, Kuo-Shyan
Bénard, François
Chen, Xiaoyuan
Kwon, Daniel
AuthorAffiliation 1 Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA; lauj2@nih.gov
2 Department of Nuclear Medicine and Radiobiology, University of Sherbrooke, Sherbrooke, QC J1H 5N4, Canada; etienne.rousseau@usherbrooke.ca
3 Department of Molecular Oncology, BC Cancer, Vancouver, BC V5Z 1L3, Canada; dkwon@bccrc.ca (D.K.); klin@bccrc.ca (K.-S.L.); fbenard@bccrc.ca (F.B.)
AuthorAffiliation_xml – name: 2 Department of Nuclear Medicine and Radiobiology, University of Sherbrooke, Sherbrooke, QC J1H 5N4, Canada; etienne.rousseau@usherbrooke.ca
– name: 3 Department of Molecular Oncology, BC Cancer, Vancouver, BC V5Z 1L3, Canada; dkwon@bccrc.ca (D.K.); klin@bccrc.ca (K.-S.L.); fbenard@bccrc.ca (F.B.)
– name: 1 Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA; lauj2@nih.gov
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  givenname: Joseph
  surname: Lau
  fullname: Lau, Joseph
  organization: Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA
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  givenname: Etienne
  orcidid: 0000-0002-2394-7446
  surname: Rousseau
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  surname: Kwon
  fullname: Kwon, Daniel
  organization: Department of Molecular Oncology, BC Cancer, Vancouver, BC V5Z 1L3, Canada
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  givenname: Kuo-Shyan
  orcidid: 0000-0002-0739-0780
  surname: Lin
  fullname: Lin, Kuo-Shyan
  organization: Department of Molecular Oncology, BC Cancer, Vancouver, BC V5Z 1L3, Canada
– sequence: 5
  givenname: François
  surname: Bénard
  fullname: Bénard, François
  organization: Department of Molecular Oncology, BC Cancer, Vancouver, BC V5Z 1L3, Canada
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  givenname: Xiaoyuan
  orcidid: 0000-0002-9622-0870
  surname: Chen
  fullname: Chen, Xiaoyuan
  organization: Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA
BackLink https://www.ncbi.nlm.nih.gov/pubmed/32455729$$D View this record in MEDLINE/PubMed
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Issue 5
Keywords radiopharmaceuticals
positron emission tomography
diagnostic imaging
radiochemistry
personalized medicine
Language English
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Snippet While the development of positron emission tomography (PET) radiopharmaceuticals closely follows that of traditional drug development, there are several key...
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Title Insight into the Development of PET Radiopharmaceuticals for Oncology
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Volume 12
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