Next Generation Radiopharmaceuticals for PET-Based Diagnostics

A special issue of Applied Sciences (ISSN 2076-3417). This special issue belongs to the section "Applied Biosciences and Bioengineering".

Deadline for manuscript submissions: closed (30 April 2022) | Viewed by 3476

Special Issue Editors


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Guest Editor
Dept of Medical Imaging, Nuclear Medicine, Radboud University Medical Center Nijmegen, Geert Grooteplein Zuid 10, 6525 GA Nijmegen, The Netherlands
Interests: radiopharmacy; radiochemistry; peptides; antibodies

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Guest Editor
1. APHM, Service de Radiopharmacie, Marseille, France
2. Aix-Marseille Univ, CNRS 2012, CERIMED, Marseille, France
3. Aix Marseille Univ, INSERM 1263, INRAE 1260, C2VN, Marseille, France
Interests: radiopharmacy; radiolabelled peptide; Preclinical imaging; Vascular imaging; theranositic

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Guest Editor
Nuclear Medicine, IRCCS Azienda Ospedaliero-Universitaria di Bologna, 40135 Bologna, Italy
Interests: PET/CT
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Special Issue Information

Dear Colleagues,

[18F]FDG was the first and main radiopharmaceutical for positron emission tomography (PET) imaging for many decades, used for imaging and measuring increased glucose metabolism in tumor cells. In the footsteps of [18F]FDG, many other first-generation radiopharmaceuticals obtained the MA, mainly used for tumor localization and staging. More recently, facing the growing need for in vivo molecular characterization as companion tools for targeted therapies as well as the new boom of the theranostic approach, PET radiopharmaceuticals have been increasingly developed as a tool for not only imaging tumors or other disease processes but also elucidating various complex biological mechanisms of tumors and metabolic and neurogenerative diseases. To allow the development of these next generation radiopharmaceuticals, new strategies have been developed. In this special issue we will discuss various new PET radiopharmaceuticals, ranging from molecular targeting strategies, pharmacokinetics optimization, development of convenient radiosynthesis, in vitro and in vivo characterization, up to their clinical applications in diagnosis.

Prof. Dr. Peter Laverman
Prof. Dr. Benjamin Guillet
Prof. Dr. Stefano Fanti
Guest Editors

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Keywords

  • Radiopharmaceuticals
  • PET
  • Imaging
  • Radiochemistry

Published Papers (1 paper)

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Review

21 pages, 2831 KiB  
Review
Phase Transfer Catalysts and Role of Reaction Environment in Nucleophilc Radiofluorinations in Automated Synthesizers
by Raisa N. Krasikova and Viktoriya V. Orlovskaya
Appl. Sci. 2022, 12(1), 321; https://0-doi-org.brum.beds.ac.uk/10.3390/app12010321 - 29 Dec 2021
Cited by 9 | Viewed by 2963
Abstract
Incorporation of [18F]fluorine into PET radiotracer structure has traditionally been accomplished via nucleophilic pathways. The [18F]fluoride is generated in an aqueous solution via proton irradiation of oxygen-18 enriched water and must to be introduced into water-free organic solutions in [...] Read more.
Incorporation of [18F]fluorine into PET radiotracer structure has traditionally been accomplished via nucleophilic pathways. The [18F]fluoride is generated in an aqueous solution via proton irradiation of oxygen-18 enriched water and must to be introduced into water-free organic solutions in order to generate reactive species. Thus nucleophilic 18F-fluorination traditionally included steps for [18F]fluoride concentration on the anion exchange resin, followed by removal of residual water via azeotropic distillation with MeCN, a time-consuming process associated with radioactivity losses and difficult automation. To circumvent this, several adsorption/elution protocols were developed based on the minimization of water content in traditional kryptofix-based [18F]fluoride eluents. The use of pre-dried KOH/kryptofix solutions, tertiary alcohols, and strong organic bases was found to be effective. Advances in transition metal-mediated SNAr approaches for radiolabeling of non-activated aromatic substrates have prompted development of alternative techniques for reactive [18F]fluoride species generation, such as organic solutions of non-basic alkyl ammonium and pyridinium sulfonates, etc. For radiofluorinations of iodonium salts precursors, a “minimalist” approach was introduced, avoiding the majority of pitfalls common to more complex methods. These innovations allowed the development of new time-efficient and convenient work-up procedures that are easily implementable in modern automated synthesizers. They will be the subject of this review. Full article
(This article belongs to the Special Issue Next Generation Radiopharmaceuticals for PET-Based Diagnostics)
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