A preliminary biodistribution study of [99mTc]sodium pertechnetate prepared from an electron linear accelerator and activated carbon-based 99mTc generator

Jang, J. S.; Kumakura, Yoshitaka; Tatenuma, Katsuyoshi; Ozeki, Atsuko; Wada, Youichiro; Akimitsu, Nobuyoshi; Tsuguchi, Akira; Kikunaga, H.; Higaki, Shogo; Uesaka, Mitsuru

doi:10.1016/j.nucmedbio.2022.03.002

Cited by 9 publications

(2 citation statements)

References 21 publications

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“…The results from the biodistribution study did not show any signs of instability for the tested tracers. Interestingly, [ 99m Tc]Tc-BQ0412, which showed release of activity under cysteine challenge in vitro, provided an adequately low activity uptake in the salivary glands and stomach (organs with a high uptake of free pertechnetate [36]), suggesting the absence of release of free technetium during catabolism in vivo. The observed difference in the excretory pathway in the biodistribution profile was not based on the hydrophilicity of the tested tracers, since they have demonstrated quite close logD values.…”

Section: Resultsmentioning

confidence: 99%

Influence of Molecular Design on the Tumor Targeting and Biodistribution of PSMA-Binding Tracers Labeled with Technetium-99m

Bezverkhniaia,

Kanellopoulos,

Rosenström

et al. 2024

IJMS

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Previously, we designed the EuK-based PSMA ligand BQ0413 with an maE3 chelator for labeling with technetium-99m. It showed efficient tumor targeting, but our preclinical data and preliminary clinical results indicated that the renal excretion levels need to be decreased. We hypothesized that this could be achieved by a decrease in the ligand’s total negative charge, achieved by substituting negatively charged glutamate residues in the chelator with glycine. The purpose of this study was to evaluate the tumor targeting and biodistribution of two new PSMA inhibitors, BQ0411 and BQ0412, compared to BQ0413. Conjugates were radiolabeled with Tc-99m and characterized in vitro, using PC3-pip cells, and in vivo, using NMRI and PC3-pip tumor-bearing mice. [99mTc]Tc-BQ0411 and [99mTc]Tc-BQ0412 demonstrated PSMA-specific binding to PC3-pip cells with picomolar affinity. The biodistribution pattern for the new conjugates was characterized by rapid excretion. The tumor uptake for [99mTc]Tc-BQ0411 was 1.6-fold higher compared to [99mTc]Tc-BQ0412 and [99mTc]Tc-BQ0413. [99mTc]Tc-BQ0413 has demonstrated predominantly renal excretion, while the new conjugates underwent both renal and hepatobiliary excretion. In this study, we have demonstrated that in such small targeting ligands as PSMA-binding EuK-based pseudopeptides, the structural blocks that do not participate in binding could have a crucial role in tumor targeting and biodistribution. The presence of a glycine-based coupling linker in BQ0411 and BQ0413 seems to optimize biodistribution. In conclusion, the substitution of amino acids in the chelating sequence is a promising method to alter the biodistribution of [99mTc]Tc-labeled small-molecule PSMA inhibitors. Further improvement of the biodistribution properties of BQ0413 is needed.

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Section: Resultsmentioning

confidence: 99%

Influence of Molecular Design on the Tumor Targeting and Biodistribution of PSMA-Binding Tracers Labeled with Technetium-99m

Bezverkhniaia,

Kanellopoulos,

Rosenström

et al. 2024

IJMS

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“…99m Tc merupakan radioisotop pemancar gamma yang memiliki energi 140 keV dan waktu paro 6 jam, dimana 99m Tc akan berada di dalam tubuh tidak begitu lama untuk mencapai organ targetnya [6][7][8][9]. 99m Tc merupakan anak radioisotop dari 99 Mo yang dapat diproduksi dengan reaksi fisi dan non fisi [10][11][12]. 99m Tc radioisotop diproduksi menggunakan sistem generator, suatu alat yang terdiri dari kolom alumina, dimana 99 Mo akan diserap ke dalam senyawa kimia berupa [ 99 Mo]MoO4 2sehingga peluruhan 99 Mo akan menjadi [ 99m Tc]TcO4 - [13][14][15].…”

Section: Pendahuluanunclassified

ESTIMASI DOSIS 99mTc-PERTEHNETAT DARI GENERATOR 99Mo / 99mTc NON-FISI PADA ANAK-ANAK USIA 1-15 TAHUN UNTUK PROSEDUR DIAGNOSTIK

Lafira,

Hidayati,

Ulya

et al. 2024

gnd

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Electron linear accelerator for medical radionuclide production

Jang

2023

Advances in Accelerators and Medical Physics

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A preliminary biodistribution study of [99mTc]sodium pertechnetate prepared from an electron linear accelerator and activated carbon-based 99mTc generator

Cited by 9 publications

References 21 publications

Influence of Molecular Design on the Tumor Targeting and Biodistribution of PSMA-Binding Tracers Labeled with Technetium-99m

Influence of Molecular Design on the Tumor Targeting and Biodistribution of PSMA-Binding Tracers Labeled with Technetium-99m

ESTIMASI DOSIS 99mTc-PERTEHNETAT DARI GENERATOR 99Mo / 99mTc NON-FISI PADA ANAK-ANAK USIA 1-15 TAHUN UNTUK PROSEDUR DIAGNOSTIK

Electron linear accelerator for medical radionuclide production

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