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Background <p>[<sup>68</sup>Ga]Ga-NODAGA[40Lys]-Exendin-4 (<sup>68</sup>Ga-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 <sup>68</sup>Ga-Ex-4 radiolabeling in sodium acetate buffer, automated on the miniAllinOne synthesizer.</p> Results <p>Key parameters were reaction volume, due to low amount of peptide, and pH. At a reaction volume of 2.65&#xa0;mL and pH 2.9, the reaction yielded 80% of <sup>68</sup>Ga-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). <sup>68</sup>Ga-Ex-4 is purified on a HLB cartridge. Final product was obtained within 40&#xa0;min, with a mean radiochemical purity of 97% and a radiochemical yield of 67%.</p> Conclusions <p>We have successfully developed a new radiolabeling method for [<sup>68</sup>Ga]Ga-NODAGA-[40Lys]Exendin-4, automated on a miniAllinOne synthesizer and using sodium acetate buffer, suitable for clinical application.</p>

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

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年6月1日

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

摘要

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.