[镥]镥-AMTG的首次人体血清稳定性研究：迈向改进的生长抑素释放肽受体靶向放射性药物治疗的一步。
First-in-Human Serum Stability Studies of [Lu]Lu-AMTG: A Step Toward Improved GRPR-Targeted Radiopharmaceutical Therapy.
作者信息
Felber Veronika, Holzleitner Nadine, Joksch Markus, Suhrbier Tim, von Amsberg Gunhild, Schwarzenböck Sarah, Kurth Jens, Heuschkel Martin, Günther Thomas, Krause Bernd J
机构信息
Department of Chemistry, TUM School of Natural Sciences, Technical University of Munich, Garching, Germany.
Department of Nuclear Medicine, Rostock University Medical Center, Rostock, Germany.
出版信息
J Nucl Med. 2025 Jun 2;66(6):896-899. doi: 10.2967/jnumed.124.269132.
The use of PET/CT with gastrin-releasing peptide receptor (GRPR) ligand [Ga]Ga-AMTG has recently been shown to diagnose metastatic disease not detected by F-PSMA PET/CT in patients with metastatic castration-resistant prostate cancer. This study aimed to analyze the serum stability of [Lu]Lu-AMTG in human subjects due to the compound's high stability observed preclinically and to elucidate its therapeutic potential. Blood samples were collected at various time points after intravenous injection of 7.6 ± 0.1 GBq of [Lu]Lu-AMTG and centrifuged. Serum samples were analyzed via reversed-phase high-performance liquid chromatography. At 1 h after injection, the mean ± SD in vivo serum stability of [Lu]Lu-AMTG was distinctly higher (62% ± 6%) than that of [Ga]Ga-RM2 (19% ± 2%). Based on the high in vivo serum stability of [Lu]Lu-AMTG in humans and favorable biodistribution, radiolabeled AMTG derivatives have the potential to improve radiopharmaceutical therapy for GRPR-expressing malignancies.
最近研究表明，使用胃泌素释放肽受体（GRPR）配体[Ga]Ga-AMTG的PET/CT能够诊断出转移性去势抵抗性前列腺癌患者中F-PSMA PET/CT未检测到的转移性疾病。本研究旨在分析[Lu]Lu-AMTG在人体受试者中的血清稳定性，因为该化合物在临床前观察到具有高稳定性，并阐明其治疗潜力。静脉注射7.6±0.1 GBq的[Lu]Lu-AMTG后，在不同时间点采集血样并离心。血清样品通过反相高效液相色谱法进行分析。注射后1小时，[Lu]Lu-AMTG的体内血清稳定性平均值±标准差明显高于[Ga]Ga-RM2（分别为62%±6%和19%±2%）。基于[Lu]Lu-AMTG在人体中的高体内血清稳定性和良好的生物分布，放射性标记的AMTG衍生物有可能改善针对表达GRPR的恶性肿瘤的放射性药物治疗。
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