Automated radiolabelling of [68Ga]Ga-PSMA-11 (gallium (68Ga)-gozetotide) using the Locametz® kit and two generators

IF 4.4 Q1 CHEMISTRY, INORGANIC & NUCLEAR EJNMMI Radiopharmacy and Chemistry Pub Date : 2024-04-17 DOI:10.1186/s41181-024-00260-4

Elke A. van Brandwijk, Else A. Aalbersberg, Arman S. Hosseini, Alwin D. R. Huitema, Jeroen J. M. A. Hendrikx

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Abstract

Background

Steps have been taken by pharmaceutical companies to obtain marketing authorisation of PSMA ligands in the European Union. Since December 2022, Locametz® (PSMA-11, gozetotide) is licensed as kit for manual radiolabelling with gallium-68 and commercially available since mid-2023. The Summary of Product Characteristic (SmPC) describes manual radiolabelling with a maximum activity after radiolabelling of 1369 MBq. We aimed for radiolabelling with a higher activity to increase production efficiency, and thus, automated radiolabelling is strongly preferred over manual radiolabelling to reduce radiation exposure to personnel. The aim of this study was to develop and validate a method for automated radiolabelling of the Locametz® kit using ~ 2000 MBq of gallium-68 eluate for radiolabelling.

Results

Automated radiolabelling of [⁶⁸Ga]Ga-PSMA-11 using the Locametz® kit provided a product which complies to the Ph. Eur., had a shelf-life of 6 h at room temperature, and theoretically reduced radiation exposure 5.7 times. Radiolabelling with one and two generator(s) resulted in a radiochemical yield of 91–102% and 96–101% after preparation, respectively. The radiochemical purity ranged from 98.0 to 99.6% for radiolabelling with one generator and ranged from 98.4 to 99.3% for radiolabelling with two generators with similar stability. The activity of the final product was much higher when using two generators, 1961–2035 MBq compared to 740–1260 MBq, which leads to ~ 1.5 times more patient syringes available per preparation.

Conclusion

Automated radiolabelling of [⁶⁸Ga]Ga-PSMA-11 using the Locametz® kit with higher gallium-68 activity than specified in the SmPC results in a product that is in compliance with the Ph. Eur. monograph and has a shelf-life of 6 h at room temperature. Radiolabelling with two generators proved possible and resulted in a product with similar quality but with much higher efficiency.

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使用 Locametz® 套件和两台发生器对[68Ga]Ga-PSMA-11（镓（68Ga）-五氮杂环丁烷）进行自动放射性标记

背景制药公司已采取措施，以获得 PSMA 配体在欧盟的上市许可。自 2022 年 12 月起，Locametz®（PSMA-11，戈再肽）作为试剂盒获得许可，可使用镓-68 进行人工放射性标记，并于 2023 年年中开始在市场上销售。产品特性摘要（SmPC）中描述的手动放射性标记后的最大活性为 1369 MBq。我们的目标是进行更高活性的放射性标记，以提高生产效率，因此，自动放射性标记比人工放射性标记更受欢迎，以减少对人员的辐射照射。本研究的目的是开发并验证一种使用约 2000 MBq 的镓-68 洗脱液对 Locametz® 试剂盒进行自动放射性标记的方法。结果使用 Locametz® 试剂盒对[68Ga]Ga-PSMA-11 进行自动放射性标记的产品符合欧洲药典，在室温下的保存期为 6 小时，理论上可减少 5.7 倍的辐射照射。使用一个和两个发生器进行放射性标记，制备后的放射化学收率分别为 91-102% 和 96-101%。使用一个发生器进行放射性标记时，放射性化学纯度为 98.0% 至 99.6%，使用两个发生器进行放射性标记时，放射性化学纯度为 98.4% 至 99.3%，稳定性相似。结论使用 Locametz® 试剂盒对[68Ga]Ga-PSMA-11 进行自动化放射性标记，镓-68 活性高于 SmPC 中的规定，得到的产品符合欧洲药典专著的要求，室温下保质期为 6 小时。使用两个发生器进行放射性标记证明是可行的，其结果是产品质量相似，但效率更高。

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