Radiosynthesis and Bioevaluation of 99mTc-Labeled Isocyanide Ubiquicidin 29-41 Derivatives as Potential Agents for Bacterial Infection Imaging

Jiang, Yuhao; Han, Peiwen; Yin, Guangxing; Wang, Qianna; Feng, Junhong; Ruan, Qing; Xiao, Di; Zhang, Junbo

doi:10.3390/ijms25021045

Cited by 3 publications

(2 citation statements)

References 55 publications

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“…Most recently, Jiang et al ( 2024 ) also aimed to improve the accumulation of 99m Tc-labelled UBI29-41 in infectious foci and, furthermore, reduce the liver uptake of the tracer by radiolabelling isocyanide UBI29-41 derivatives (CNnUBI29-41; n = 5–9; see Fig. 10 ) with different 99m Tc cores, i.e.…”

Section: Main Textmentioning

confidence: 99%

“…Conventional infection imaging agents (such as [ 67 Ga]Ga-citrate, [ 111 In]In-oxine- or [ 99m Tc]Tc-HMPAO-labelled leukocytes, and [ 18 F]FDG) do not target bacteria, but rather the host immune response to the bacterial infection, and will therefore also localise in sterile inflammatory foci. The nonspecificity of these tracers can result in delayed or even inaccurate diagnosis, localisation, and treatment of infection, which may increase the cost-related burden, antimicrobial resistance, morbidity and even mortality of patients (Jiang et al 2024 ; Margeta et al 2024 ; Santos et al 2024 ; Spoelstra et al 2024 ; Li et al 2020 ). The development and investigation of new radiopharmaceuticals focuses on the differentiation of infection from sterile inflammation and the imaging of specific infectious microbes and processes (Palestro 2019 ; Signore et al 2022 ).…”

Section: Introductionmentioning

confidence: 99%

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Recently developed radiopharmaceuticals for bacterial infection imaging

Kahts,

Summers,

Gutta

et al. 2024

EJNMMI radiopharm. chem.

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Background Infection remains a major cause of morbidity and mortality, regardless of advances in antimicrobial therapy and improved knowledge of microorganisms. With the major global threat posed by antimicrobial resistance, fast and accurate diagnosis of infections, and the reliable identification of intractable infection, are becoming more crucial for effective treatment and the application of antibiotic stewardship. Molecular imaging with the use of nuclear medicine allows early detection and localisation of infection and inflammatory processes, as well as accurate monitoring of treatment response. There has been a continuous search for more specific radiopharmaceuticals to be utilised for infection imaging. This review summarises the most prominent discoveries in specifically bacterial infection imaging agents over the last five years, since 2019. Main body Some promising new radiopharmaceuticals evaluated in patient studies are reported here, including radiolabelled bacterial siderophores like [68Ga]Ga-DFO-B, radiolabelled antimicrobial peptide/peptide fragments like [68Ga]Ga-NOTA-UBI29-41, and agents that target bacterial synthesis pathways (folic acid and peptidoglycan) like [11C]para-aminobenzoic acid and D-methyl-[11C]-methionine, with clinical trials underway for [18F]fluorodeoxy-sorbitol, as well as for 11C- and 18F-labelled trimethoprim. Conclusion It is evident that a great deal of effort has gone into the development of new radiopharmaceuticals for infection imaging over the last few years, with remarkable progress in preclinical investigations. However, translation to clinical trials, and eventually clinical Nuclear Medicine practice, is apparently slow. It is the authors’ opinion that a more structured and harmonised preclinical setting and well-designed clinical investigations are the key to reliably evaluate the true potential of the newly proposed infection imaging agents.

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Section: Main Textmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Recently developed radiopharmaceuticals for bacterial infection imaging

Kahts,

Summers,

Gutta

et al. 2024

EJNMMI radiopharm. chem.

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A brief overview of common radiopharmaceuticals for detection of infection/inflammation in nuclear medicine

Vahidfar,

Farzanefar,

Bakhshi Kashi

et al. 2024

J Radioanal Nucl Chem

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Application of 99mTc-Labeled WL12 Peptides as a Tumor PD-L1-Targeted SPECT Imaging Agent: Kit Formulation, Preclinical Evaluation, and Study on the Influence of Coligands

Fan,

Yao,

Zhao

et al. 2024

Pharmaceuticals

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With the development of PD-1/PD-L1 immune checkpoint inhibitor therapy, the ability to monitor PD-L1 expression in the tumor microenvironment is important for guiding therapy. This study was performed to develop a novel radiotracer with optimal pharmacokinetic properties to reflect PD-L1 expression in vivo via single-photon emission computed tomography (SPECT) imaging. [99mTc]Tc-HYNIC-WL12-tricine/M (M = TPPTS, PDA, ISONIC, 4-PSA) complexes with high radiochemical purity (>97%) and suitable molar activity (from 100.5 GBq/μmol to 300 GBq/μmol) were prepared through a kit preparation process. All 99mTc-labeled HYNIC-WL12 radiotracers displayed good in vitro stability for 4 h. The affinity and specificity of the four radiotracers for PD-L1 were demonstrated both in vitro and in vivo. The results of biodistribution studies displayed that the pharmacokinetics of the 99mTc-HYNIC-conjugated radiotracers were significantly influenced by the coligands of the radiotracers. Among them, [99mTc]Tc-HYNIC-WL12-tricine/ISONIC exhibited the optimal pharmacokinetic properties (t1/2α = 8.55 min, t1/2β = 54.05 min), including the fastest clearance in nontarget tissues, highest tumor-to-background contrast (e.g., tumor-to-muscle ratio, tumor-to-blood ratio: 40.42 ± 1.59, 14.72 ± 2.77 at 4 h p.i., respectively), and the lowest estimated radiation absorbed dose, highlighting its potential as a clinical SPECT imaging probe for tumor PD-L1 detection.

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Radiosynthesis and Bioevaluation of 99mTc-Labeled Isocyanide Ubiquicidin 29-41 Derivatives as Potential Agents for Bacterial Infection Imaging

Cited by 3 publications

References 55 publications

Recently developed radiopharmaceuticals for bacterial infection imaging

Recently developed radiopharmaceuticals for bacterial infection imaging

A brief overview of common radiopharmaceuticals for detection of infection/inflammation in nuclear medicine

Application of 99mTc-Labeled WL12 Peptides as a Tumor PD-L1-Targeted SPECT Imaging Agent: Kit Formulation, Preclinical Evaluation, and Study on the Influence of Coligands

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