Evaluating the potential of kit-based 68Ga-ubiquicidin formulation in diagnosis of infection

Bhusari, Priya; Bhatt, Jyotsna; Sood, Apurva; Kaur, Ruchikapreet; Vatsa, Rakhee; Rastogi, Ashu; Mukherjee, Archana; Dash, Ashutosh; Mittal, Bhagwant Rai; Shukla, Jaya

doi:10.1097/mnm.0000000000000943

Cited by 17 publications

(22 citation statements)

References 13 publications

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“… 52 Themain advantage of radionuclides over FPs and fluorescent organic probes for peptide labeling is their reduced size ( Figure 3 ). The AMP ubiquicidin (UBI), for example, displays low toxicity toward mammalian cells, binds specifically to the bacterial cell membrane, and is widely used in nuclear imaging for infection detection when labeled with 68 Ga. 53 - 56 UBI has been functionalized with a chelator (1,4,7-triazacyclononane-1,4,7-triacetic acid [NOTA]) and complexed with 68 Ga to study its cytotoxicity in vitro , in addition to its biodistribution, pharmacokinetics, and radiation dosimetry in non-human primates. These results led to the first-in-human evaluation of infection diagnosis using PET/CT imaging.…”

Section: Introductionmentioning

confidence: 99%

Light-Emitting Probes for Labeling Peptides

Boaro

Ageitos

Torres

et al. 2020

Cell Reports Physical Science

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SUMMARY Peptides are versatile biopolymers composed of 2–100 amino acid residues that present a wide range of biological functions and constitute potential therapies for numerous diseases, partly due to their ability to penetrate cell membranes. However, their mechanisms of action have not been fully elucidated due to the lack of appropriate tools. Existing light-emitting probes are limited by their cytotoxicity and large size, which can alter peptide structure and function. Here, we describe the available fluorescent, bioluminescent, and chemiluminescent probes for labeling peptides, with a focus on minimalistic options.

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Section: Introductionmentioning

confidence: 99%

Light-Emitting Probes for Labeling Peptides

Boaro

Ageitos

Torres

et al. 2020

Cell Reports Physical Science

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“…It was first labeled with 99m Tc ( 197 ). A 68 Ga-PET surrogate has subsequently been developed and investigated using a kit-based preparation ( 153 ). This small study on 10 patients gave mixed results, as 4 patients gave false negative results possibly because of antibiotic treatment (2 patients) or because of very low microbial population.…”

Section: Cold Kitsmentioning

confidence: 99%

Cold Kit Labeling: The Future of 68Ga Radiopharmaceuticals?

Lepareur

2022

Front. Med.

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Over the last couple of decades, gallium-68 (68Ga) has gained a formidable interest for PET molecular imaging of various conditions, from cancer to infection, through cardiac pathologies or neuropathies. It has gained routine use, with successful radiopharmaceuticals such as somatostatin analogs ([68Ga]Ga-DOTATOC and [68Ga]GaDOTATATE) for neuroendocrine tumors, and PSMA ligands for prostate cancer. It represents a major clinical impact, particularly in the context of theranostics, coupled with their 177Lu-labeled counterparts. Beside those, a bunch of new 68Ga-labeled molecules are in the preclinical and clinical pipelines, with some of them showing great promise for patient care. Increasing clinical demand and regulatory issues have led to the development of automated procedures for the production of 68Ga radiopharmaceuticals. However, the widespread use of these radiopharmaceuticals may rely on simple and efficient radiolabeling methods, undemanding in terms of equipment and infrastructure. To make them technically and economically accessible to the medical community and its patients, it appears mandatory to develop a procedure similar to the well-established kit-based 99mTc chemistry. Already available commercial kits for the production of 68Ga radiopharmaceuticals have demonstrated the feasibility of using such an approach, thus paving the way for more kit-based 68Ga radiopharmaceuticals to be developed. This article discusses the development of 68Ga cold kit radiopharmacy, including technical issues, and regulatory aspects.

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“…22 Case-reports and case-series of human use. 23,24 Sequential 99m Tc-UBI 29-41 scintigraphy before and after antibiotic therapy correlated with clinical outcomes in a patient cohort. 25 Journal of Medicinal Chemistry and are recognized and taken up by active transporters of the microorganism.…”

Section: -18mentioning

confidence: 99%