Radiosynthesis Standardization and Preclinical Assessment of the [[sup.68]Ga]Ga-DOTA-Ubiquicidin[sub.29-41]: A Translational Study Targeting Differential Diagnosis of Infectious Processes

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. Howev...

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Published in:Pharmaceuticals (Basel, Switzerland) Switzerland), 2023-12, Vol.17 (1)
Main Authors: Miranda, Ana Cláudia Camargo, Fuscaldi, Leonardo Lima, Mejia, Jorge, da Silva, Fábio Fernando Alves, Turato, Walter Miguel, Mendonça, Fernanda Ferreira, Nogueira, Solange Amorim, Osawa, Akemi, Yamaga, Lilian Yuri Itaya, Malavolta, Luciana, de Barboza, Marycel Figols
Format: Article
Language:English
Subjects:
Bacterial infections
Diagnosis
Diagnosis, Differential
Methods
Radiopharmaceuticals
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Summary: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, [[sup.68] Ga]Ga-DOTA-Ubiquicidin[sub.29-41] 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 [[sup.68] Ga]Ga-DOTA-Ubiquicidin[sub.29-41] as a radiopharmaceutical that can be obtained in a hospital radiopharmacy for the diagnosis of infectious processes using PET/CT.
ISSN:1424-8247
1424-8247
DOI:10.3390/ph17010048