Monitoring the efficacy of antibacterial treatments of infections with Tc-99m labelled antimicrobial peptides

Nibbering, Peter H.; Welling, Mick M.; Paulusma-Annema, Akke; Barselaar, M. T. Van Den; Pauwels, E. K. J.

doi:10.1097/00006231-200006000-00060

Cited by 9 publications

(7 citation statements)

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“…Ubiquicidin (UBI) is a human antimicrobial peptide and synthetic derivatives of this peptide have been suggested as a possible agent for imaging infections [12,13]. The UBI fragment 29-41 (TGRAKRRMQYNRR) has been successfully labelled with technetium-99m [14,15]. As mentioned previously, better spatial resolution can be obtained using PET radionuclides such as gallium-68, as opposed to technetium-99m, a conventional SPECT radionuclide.…”

Section: Theorymentioning

confidence: 99%

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An automated synthesis method for 68Ga-labelled ubiquicidin 29–41

Rubow

Ebenhan

et al. 2019

J Radioanal Nucl Chem

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Published methods for radiolabelling of 1,4,7-triazacyclononane-1,4,7-triacetic acid ubiquicidin (NOTA-UBI) 29-41 to date describe manual or kit-based procedures. The purpose of this study was to develop an automated synthesis method for the synthesis of [ 68 Ga]Ga-NOTA-UBI. NOTA-UBI was successfully labelled with gallium-68 using the three different automated procedures. The use of radical scavengers to improve radiochemical purity is also discussed. The automated procedures showed a high degree of robustness and repeatability. The validated automated synthesis protocols using a Scintomics GRP Module will contribute to provide GMP-compliant [ 68 Ga]Ga-NOTA-UBI for clinical infection imaging.

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Section: Theorymentioning

confidence: 99%

“…Published methods for radiolabelling of UBI initially only d manual processes [14,15,21,22]. More recently, kit-based labelling methods have also been published [23,24].…”

Section: Theorymentioning

confidence: 99%

An automated synthesis method for 68Ga-labelled ubiquicidin 29–41

Rubow

Ebenhan

et al. 2019

J Radioanal Nucl Chem

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“…The antibacterial effect was found to be associated with an increased influx of neutrophils into the infected area [ 134 ]. Use of this agent in experimental thigh muscle infection in mice allowed rapid visualization of bacterial infections, but abscess to background ratios were low and decreased with time [ 135 , 136 ].…”

Section: Key Features Of Antimicrobial Peptidesmentioning

confidence: 99%

Antimicrobial Peptides as Infection Imaging Agents: Better Than Radiolabeled Antibiotics

Akhtar¹,

Imran²,

Nadeem³

et al. 2012

International Journal of Peptides

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Nuclear medicine imaging techniques offer whole body imaging for localization of number and site of infective foci inspite of limitation of spatial resolution. The innate human immune system contains a large member of important elements including antimicrobial peptides to combat any form of infection. However, development of antibiotics against bacteria progressed rapidly and gained popularity over antimicrobial peptides but even powerful antimicrobials failed to reduce morbidity and mortality due to emergence of mutant strains of bacteria resulting in antimicrobial resistance. Differentiation between infection and inflammation using radiolabeled compounds with nuclear medicine techniques has always been a dilemma which is still to be resolved. Starting from nonspecific tracers to specific radiolabeled tracers, the question is still unanswered. Specific radiolabeled tracers included antibiotics and antimicrobial peptides which bind directly to the bacteria for efficient localization with advanced nuclear medicine equipments. However, there are merits and demerits attributed to each. In the current paper, radiolabeled antibiotics and radiolabeled peptides for infection localization have been discussed starting with the background of primitive nonspecific tracers. Radiolabeled antimicrobial peptides have certain merits compared with labeled antibiotics which make them superior agents for localization of infective focus.

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“…The UBI 29-41 fragment was previously radiolabeled with 99m Tc, a gamma emitter, for SPECT imaging in clinical routine [26,27]. Nowadays, 68 Ga-labeled molecules have been developed due to some of its properties, such as being classified as a trivalent metal with a physical half-life of 67.71 min, which is consistent with the biodistribution time of low molecular weight peptides such as UBI [29][30][31][32][33][34][35][36][37][38][39][40][41] , and being readily available, via a generator system, for use in PET via radiopharmaceutical production in a hospital radiopharmacy [2,28].…”

Section: Introductionmentioning

confidence: 99%

Radiosynthesis Standardization and Preclinical Assessment of the [68Ga]Ga-DOTA-Ubiquicidin29-41: A Translational Study Targeting Differential Diagnosis of Infectious Processes

Miranda,

Fuscaldi,

Mejia

et al. 2023

Pharmaceuticals

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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.

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Monitoring the efficacy of antibacterial treatments of infections with Tc-99m labelled antimicrobial peptides

Cited by 9 publications

References 0 publications

An automated synthesis method for 68Ga-labelled ubiquicidin 29–41

An automated synthesis method for 68Ga-labelled ubiquicidin 29–41

Antimicrobial Peptides as Infection Imaging Agents: Better Than Radiolabeled Antibiotics

Radiosynthesis Standardization and Preclinical Assessment of the [68Ga]Ga-DOTA-Ubiquicidin29-41: A Translational Study Targeting Differential Diagnosis of Infectious Processes

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