Development of an automated radiosynthesis for [68Ga]Ga-NODAGA[40Lys]-Exendin-4 in sodium acetate buffer

IF 3.7 Q1 CHEMISTRY, INORGANIC & NUCLEAR

EJNMMI Radiopharmacy and Chemistry Pub Date : 2026-06-01 Epub Date: 2026-08-05 DOI:10.1186/s41181-026-00452-0

Maïlys Ragot, Pauline Reynaud-Orhon, Alban Revy, Marie Batisse-Lignier, Valentin Brusseau, Antony Kelly, Hosameldin Otman, Florent Cachin, Marion Chanchou, Sophie Levesque, Marion Tempier

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Abstract

Background

[⁶⁸Ga]Ga-NODAGA[40Lys]-Exendin-4 (⁶⁸Ga-Ex-4) is a new PET radiopharmaceutical targeting GLP-1-R that showed great specificity and sensitivity in the topographic diagnosis of benign insulinoma. We herein report the development of a new method for ⁶⁸Ga-Ex-4 radiolabeling in sodium acetate buffer, automated on the miniAllinOne synthesizer.

Results

Key parameters were reaction volume, due to low amount of peptide, and pH. At a reaction volume of 2.65 mL and pH 2.9, the reaction yielded 80% of ⁶⁸Ga-Ex-4. The use of polysorbate and cooling of the solution allows to decrease the adsorption on the reaction vial (from 29 to 2% of total activity remaining on the vial). ⁶⁸Ga-Ex-4 is purified on a HLB cartridge. Final product was obtained within 40 min, with a mean radiochemical purity of 97% and a radiochemical yield of 67%.

Conclusions

We have successfully developed a new radiolabeling method for [⁶⁸Ga]Ga-NODAGA-[40Lys]Exendin-4, automated on a miniAllinOne synthesizer and using sodium acetate buffer, suitable for clinical application.

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醋酸钠缓冲液中[68Ga]Ga-NODAGA[40Lys]-Exendin-4的自动放射性合成

背景：[68Ga]Ga-NODAGA[40Lys]-Exendin-4 （68Ga- ex -4）是一种靶向GLP-1-R的新型PET放射性药物，在良性胰岛素瘤的影像学诊断中具有很高的特异性和敏感性。本文报道了一种在醋酸钠缓冲液中进行68Ga-Ex-4放射性标记的新方法，该方法在miniAllinOne合成器上自动进行。结果：关键参数为反应体积和pH，因为多肽量少。反应体积为2.65 mL， pH为2.9时，68Ga-Ex-4的收率为80%。使用聚山梨酸酯和冷却溶液可以减少反应瓶上的吸附（从瓶上剩余总活性的29%到2%）。68Ga-Ex-4在HLB滤筒上纯化。最终产物在40分钟内获得，平均放射化学纯度为97%，放射化学产率为67%。结论：我们成功开发了一种新的[68Ga]Ga-NODAGA-[40Lys]Exendin-4的放射性标记方法，该方法在miniAllinOne合成器上自动化，使用醋酸钠缓冲液，适合临床应用。

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