Osteotropic radiopharmaceuticals in Russian nuclear medicine techniques

Кодина, Г. Е.; Malysheva, A. O.; Klement'eva, O.

doi:10.1007/s11172-016-1308-0

Cited by 7 publications

(3 citation statements)

References 21 publications

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“…Figure 3 shows the ligand concentration-labelling reaction yield dependence for the ligand 9 and previously studied 1,7-diamino-4-oxaheptane-1,1,7,7-tetraphosphonic acid (1) [10]. The conditions of 68 Ga-labelling for both compounds were the same: рН6, acetate concentration of 0.2 M, 25 • C, and 15 min reaction time.…”

Section: Radiolabelling and Stabilitymentioning

confidence: 99%

“…Many studies are devoted to the search of osteotropic 68 Ga radiopharmaceuticals Molecules 2021, 26, 2357 2 of 14 for imaging bone metastases during the early stages [6][7][8][9]. Phosphonate ligands are commonly used for this purpose as they work with other radionuclides ( 99m Tc, 111 In, 153 Sm, 188 Re) [10,11]. 1-Amino-1,1-diphosphonic acids having fine complexation properties are of interest as ligands for radiopharmaceuticals.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis, Complexation Properties, and Evaluation of New Aminodiphosphonic Acids as Vector Molecules for 68Ga Radiopharmaceuticals

et al. 2021

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Two new aminodiphosphonic acids derived from salicylic acid and its phosphonic analogue were prepared through a simple and efficient synthesis. 2-[(2-Amino-2,2-diphosphono)ethyloxy]-benzoic acid 8 and 2-[(2-amino-2,2-diphosphono)ethyloxy]-5-ethyl-phenylphosphonic acid 9 were evaluated for their applicability as 68Ga binding bone-seeking agents. Protonation constants of 8 and 9 and stability constants of the Ga3+ complexes with 8 and 9 in water were determined. The stability constant of Ga3+ complex with fully phosphorylated acid 9 (logKGaL = 31.92 ± 0.32) significantly exceeds stability constant of Ga3+ complex with 8 (logKGaL = 26.63 ± 0.24). Ligands 8 and 9 are as effective for Ga3+ cation binding as ethylenediamine-N,N’-diacetic-N,N’-bis(methy1enephosphonic) acid and ethylenediamine-N,N,N’,N’-tetrakis(methylenephosphonic) acid, respectively. The labelling process and stability of [68Ga]Ga-8 and [68Ga]Ga-9 were studied. Both 8 and 9 readily form 68Ga-complexes stable to ten-fold dilution with saline. However, in fetal bovine serum, only [68Ga]Ga-9 was stable enough to be subject to biological evaluation. It was injected into rats with bone pathology and aseptic inflammation of soft tissues. For [68Ga]Ga-9 in animals with a bone pathology model in 60 and 120 min after injection, a slight accumulation in the pathology site, stable blood percentage level, and moderate accumulation in the liver were observed. For animals with an aseptic inflammation, the accumulation of [68Ga]Ga-9 in the pathology site was higher than that in animals with bone pathology. Moreover, the accumulation of [68Ga]Ga-9 in inflammation sites was more stable than that for [68Ga]Ga-citrate. The percentage of [68Ga]Ga-9 in the blood decreased from 3.1% ID/g (60 min) to 1.5% ID/g (120 min). Accumulation in the liver was comparable to that obtained for [68Ga]Ga-citrate.

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Section: Radiolabelling and Stabilitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis, Complexation Properties, and Evaluation of New Aminodiphosphonic Acids as Vector Molecules for 68Ga Radiopharmaceuticals

et al. 2021

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“…Было показано, Ga» был синтезирован на основе оксабифора -оксабис(этиленнитрило)тетраметиленфосфоновой кислоты (рис. 2)[34]. Содержание активности в скелете лабораторных животных через 1 ч после введения достигало 30,3% от введённой дозы.…”

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Bone-seeking radiopharmaceuticals based on phosphonic acids and Ga-68 (review)

Tishchenko¹,

Петриев²,

Zavestovskaya³

et al. 2020

Radiation and Risk

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Костные метастазы-наиболее частое осложнение некоторых солидных опухолей, особенно на поздних стадиях. Среди всех локализаций метастазов злокачественных опухолей кости занимают третье место по частоте после печени и лёгких. Подавляющее большинство метастатических изменений в костях происходит из опухолей молочной железы, предстательной железы и лёгких [1, 2]. Более половины пациентов с костными метастазами страдают от болей в костях, существенно ухудшающих качество их жизни. Кроме того, несвоевременная диагностика или неправильное лечение могут привести к таким серьёзным осложнениям, как компрессия спинного мозга, гиперкальциемия и патологические переломы различных костей [3]. Поэтому раннее выявление и адекватная терапия метастазов в костях обеспечивает максимальное повышение качества жизни пациента и его функциональную активность. Решение этой проблемы связывают, прежде всего, с развитием метода позитронноэмиссионной томографии (ПЭТ), потенциал которого в значительной степени определяется ар

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