Synthesis and quality control of [225Ac][Ac-DOTATATE]: feasibility of the targeted alpha therapy (TAT) in conventional clinical pharmacy equipped for Tc-99 m in Pakistan

IF 1.6 3区化学 Q3 CHEMISTRY, ANALYTICAL

Journal of Radioanalytical and Nuclear Chemistry Pub Date : 2025-08-30 DOI:10.1007/s10967-025-10346-1

Shakera Khatoon Rizvi, Amna Javed, Qaiser Khan

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Abstract

Actinium-225-labeled DOTATATE is a promising candidate for targeted alpha therapy (TAT) of neuroendocrine tumors due to its favorable radionuclide properties and ease of synthesis. This study evaluates the feasibility of using standard QC methods, typically used for Tc-99 m, for TAT with Ac-225. [225Ac][Ac-DOTATATE] was synthesized with > 92 ± 2% radiochemical purity and the product remained stable for 24 h. Gamma spectrometry showed > 99.9% radionuclide purity. ITLC-SG paper in aqueous acetonitrile resolved radiochemical species effectively, with Rf values of 0.2 for free radiometal and 0.8–0.9 for the labeled peptide while opposite behavior was observed with sodium citrate as mobile phase. These results demonstrate that standard QC infrastructure in Pakistan is adequate for alpha therapy, facilitating routine clinical application.

Graphical abstract

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[225Ac][Ac-DOTATATE]的合成与质量控制：靶向α治疗（TAT）在巴基斯坦Tc-99 m常规临床药房的可行性

由于其良好的放射性核素性质和易于合成，锕-225标记的DOTATATE是神经内分泌肿瘤靶向α治疗（TAT）的有希望的候选者。本研究评估了使用标准QC方法的可行性，通常用于Tc-99 m，用于Ac-225的TAT。合成的[225Ac][Ac-DOTATATE]的放射化学纯度为>； 92±2%，产物保持稳定24 h，伽马能谱显示放射性核素纯度为>； 99.9%。ITLC-SG纸在乙腈水溶液中有效地溶解了放射性化学物质，游离放射性金属的Rf值为0.2，标记肽的Rf值为0.8-0.9，而柠檬酸钠为流动相时则相反。这些结果表明，巴基斯坦标准的QC基础设施足以用于α治疗，促进了常规临床应用。图形抽象

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来源期刊

Journal of Radioanalytical and Nuclear Chemistry 化学-分析化学

CiteScore

2.80

自引率

18.80%

发文量

504

审稿时长

2.2 months

期刊介绍： An international periodical publishing original papers, letters, review papers and short communications on nuclear chemistry. The subjects covered include: Nuclear chemistry, Radiochemistry, Radiation chemistry, Radiobiological chemistry, Environmental radiochemistry, Production and control of radioisotopes and labelled compounds, Nuclear power plant chemistry, Nuclear fuel chemistry, Radioanalytical chemistry, Radiation detection and measurement, Nuclear instrumentation and automation, etc.