Jagodziński Michał, Boratyński Jakub, Hamankiewicz Paulina, Cheda Łukasz, Uhrynowski Witold, Girstun Agnieszka, Trzcińska-Danielewicz Joanna, Rogulski Zbigniew, Pilch-Kowalczyk Marek
VOXEL S.A, Radiopharmaceutical Production Center, ul. Wrocławska 1-3, 30-006 Kraków, Poland.
University of Warsaw, Faculty of Chemistry, Pasteura 1, 02-093 Warsaw, Poland.
Molecules. 2025 Aug 22;30(17):3458. doi: 10.3390/molecules30173458.
Gallium-68 is a widely used positron-emitting radionuclide in nuclear medicine, traditionally obtained from Ge/Ga generators. However, increasing clinical demand has driven interest in alternative production methods, such as medical cyclotrons equipped with solid targets. This study evaluates the functional equivalence of gallium-68 chloride obtained from cyclotron solid target and formulated to be equivalent to the eluate from a germanium-gallium generator, aiming to determine whether this production method can serve as a reliable alternative for PET radiopharmaceutical applications. Preparations of [Ga]Ga-PSMA-11 and [Ga]Ga-DOTATOC, labeled with cyclotron-derived gallium-68 chloride, were subjected to quality control analysis using radio thin layer chromatography and radio high performance liquid chromatography. Subsequently, biodistribution studies were performed in mouse oncological models of expression of PSMA antigen and SSTR receptor to compare uptake of preparations produced with generator and cyclotron-derived isotopes. All tested formulations met the required radiochemical purity specifications. Moreover, tumor accumulation of the radiolabeled compounds was comparable regardless of the isotope source. The results support the conclusion that gallium-68 produced via cyclotron is functionally equivalent to that obtained from a generator, demonstrating its potential for interchangeable use in clinical and research radiopharmaceutical applications.
镓-68是核医学中广泛使用的正电子发射放射性核素，传统上是从锗/镓发生器中获得的。然而，临床需求的不断增加引发了人们对替代生产方法的兴趣，例如配备固体靶的医用回旋加速器。本研究评估了从回旋加速器固体靶获得并配制得与锗-镓发生器洗脱液等效的氯化镓-68的功能等效性，旨在确定这种生产方法是否可作为正电子发射断层显像（PET）放射性药物应用的可靠替代方法。使用放射性薄层色谱法和放射性高效液相色谱法对用回旋加速器衍生的氯化镓-68标记的[镓]镓-PSMA-11和[镓]镓- DOTATOC制剂进行质量控制分析。随后，在表达PSMA抗原和SSTR受体的小鼠肿瘤模型中进行生物分布研究，以比较用发生器和回旋加速器衍生的同位素生产的制剂的摄取情况。所有测试制剂均符合所需的放射化学纯度规格。此外，无论同位素来源如何，放射性标记化合物的肿瘤蓄积情况相当。结果支持以下结论：通过回旋加速器生产的镓-68在功能上等同于从发生器获得的镓-68，表明其在临床和研究放射性药物应用中可互换使用的潜力。
