Gallium 68 Radiochemistry and Labelling Strategies

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Radiopharmaceutical Sciences".

Deadline for manuscript submissions: closed (20 February 2024) | Viewed by 2436

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Department of Molecular and Medical Pharmacology, University of California, Los Angeles, CA 90095, USA
Interests: metabolism and cancer; nuclear medicine; radiochemistry
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Guest Editor
Department of Surgical Science, Uppsala University, 751 85 Uppsala, Sweden
Interests: nuclear medicine; radiochemistry; positron emission tomography; molecular imaging; radiopharmaceutical sciences; cancer; diabetes; fibrosis; drug development; inflammation
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Special Issue Information

Dear Colleagues,

Gallium-68 (68Ga) has proven to be an essential radionuclide for the fundamental biological studies, development of radiopharmaceuticals for clinical use, and drug development due to its favorable physical and chemical properties as well as ready availability from a generator system. The interest in 68Ga has increased tremendously in the recent decade as a result of wide clinical applications in combination with positron emission tomography (PET) and its connection to the subsequent radiotherapy in the context of (radio)theranostics. The crucial advantages of 68Ga are its availability from a 68Ge/68Ga generator and its labelling chemistry amenable to the automation and kit-type preparation. Moreover, it can nowadays also be produced with a cyclotron using solid and liquid targets.

This Special Issue will focus on the development of 68Ga radiopharmaceuticals and their applications. The subject may range from radioactive isotope production, labeling chemistry and quality control to preclinical evaluation and clinical trials and clinical routine application. The (radio)theranostic and pharmacokinetic modelling studies are also of strong interest.

Dr. Giuseppe Carlucci
Dr. Irina Velikyan
Guest Editors

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Keywords

  • radionuclide Gallium-68 (radioisotopes)
  • radiolabeling
  • quality control (radiopharmaceuticals)
  • radiopharmaceutical pK/pD (radiotracer)
  • theranostics (diagnostics and therapeutics)
  • molecular imaging

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Published Papers (1 paper)

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Research

14 pages, 3502 KiB  
Article
Radiosynthesis Standardization and Preclinical Assessment of the [68Ga]Ga-DOTA-Ubiquicidin29-41: A Translational Study Targeting Differential Diagnosis of Infectious Processes
by Ana Cláudia Camargo Miranda, Leonardo Lima Fuscaldi, Jorge Mejia, Fábio Fernando Alves da Silva, Walter Miguel Turato, Fernanda Ferreira Mendonça, Solange Amorim Nogueira, Akemi Osawa, Lilian Yuri Itaya Yamaga, Luciana Malavolta and Marycel Figols de Barboza
Pharmaceuticals 2024, 17(1), 48; https://doi.org/10.3390/ph17010048 - 28 Dec 2023
Viewed by 1622
Abstract
Human bacterial infections significantly contribute to the increase in healthcare-related burdens. This scenario drives the study of novel techniques for the early and precise diagnosis of infectious processes. Some alternatives include Nuclear Medicine- and Molecular Imaging-based strategies. However, radiopharmaceuticals that are available for [...] Read more.
Human bacterial infections significantly contribute to the increase in healthcare-related burdens. This scenario drives the study of novel techniques for the early and precise diagnosis of infectious processes. Some alternatives include Nuclear Medicine- and Molecular Imaging-based strategies. However, radiopharmaceuticals that are available for routine assessments are not specific to differentiating infectious from aseptic inflammatory processes. In this context, [68Ga]Ga-DOTA-Ubiquicidin29-41 was synthesized using an automated module and radiochemical; in vivo and in vitro studies were performed. The radiopharmaceutical remained stable in saline (up to 180 min) and in rodent serum (up to 120 min) with radiochemical purities > 99 and 95%, respectively. Partition coefficient and serum protein binding at 60 min were determined (−3.63 ± 0.17 and 44.06 ± 1.88%, respectively). Ex vivo biodistribution, as well as in vivo microPET/CT images in mice, showed rapid blood clearance with renal excretion and reduced uptake in other organs in Staphylococcus aureus-infected animals. Higher uptake was observed in the target as compared to the non-target tissue (p < 0.0001) at 60 min post administration. The presented in-human clinical case demonstrates uptake of the radiopharmaceutical by Staphyloccocus aureus bacteria. These results indicate the potential of [68Ga]Ga-DOTA-Ubiquicidin29-41 as a radiopharmaceutical that can be obtained in a hospital radiopharmacy for the diagnosis of infectious processes using PET/CT. Full article
(This article belongs to the Special Issue Gallium 68 Radiochemistry and Labelling Strategies)
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