van Brandwijk Elke A, Aalbersberg Else A, Hosseini Arman S, Huitema Alwin D R, Hendrikx Jeroen J M A
Department of Nuclear Medicine, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX, Amsterdam, The Netherlands.
Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute, Amsterdam, The Netherlands.
EJNMMI Radiopharm Chem. 2024 Apr 17;9(1):31. doi: 10.1186/s41181-024-00260-4.
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.
Automated radiolabelling of [Ga]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.
Automated radiolabelling of [Ga]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.
制药公司已采取措施在欧盟获取前列腺特异性膜抗原（PSMA）配体的上市许可。自2022年12月起，Locametz®（PSMA - 11，戈泽托肽）被许可作为用镓 - 68进行手动放射性标记的试剂盒，并自2023年年中起可商购。产品特性摘要（SmPC）描述了手动放射性标记，放射性标记后的最大活度为1369 MBq。我们旨在进行更高活度的放射性标记以提高生产效率，因此，相较于手动放射性标记，强烈推荐使用自动放射性标记以减少人员的辐射暴露。本研究的目的是开发并验证一种使用约2000 MBq镓 - 68洗脱液对Locametz®试剂盒进行自动放射性标记的方法。
使用Locametz®试剂盒对[Ga]Ga - PSMA - 11进行自动放射性标记得到的产品符合欧洲药典，在室温下保质期为6小时，理论上辐射暴露减少了5.7倍。使用一台和两台发生器进行放射性标记，制备后放射化学产率分别为91 - 102%和96 - 101%。使用一台发生器进行放射性标记时，放射化学纯度范围为98.0%至99.6%，使用两台发生器进行放射性标记时，放射化学纯度范围为98.4%至99.3%，稳定性相似。使用两台发生器时最终产品的活度要高得多，为1961 - 2035 MBq，而使用一台发生器时为740 - 1260 MBq，这使得每次制备可提供的患者注射器数量增加约1.5倍。
使用Locametz®试剂盒对[Ga]Ga - PSMA - 11进行自动放射性标记，使用比SmPC规定更高活度的镓 - 68，得到的产品符合欧洲药典专论，在室温下保质期为6小时。使用两台发生器进行放射性标记被证明是可行的，得到的产品质量相似但效率更高。
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