Development and validation of a kit formulation of [68Ga] Ga-P15-041 as a bone imaging agent
Development and validation of a kit formulation of [68Ga] Ga-P15-041 as a bone imaging agent
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DOI：
10.1016/j.apradiso.2020.109485
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发表时间：
2021-03-01
影响因子：
1.6
通讯作者：
Kung, Hank F.
中科院分区：
文献类型：
--
作者：
Hong, Haiyan;Ploessl, Karl;Kung, Hank F.
在核医学中通常进行的研究之一是使用[Tc-99 m] Tc-亚甲基二膦酸盐（MDP）进行骨扫描，用于检测各种骨病变，包括癌症转移。最近出现的市售Ge-68/Ga-68放射性核素发生器使得有可能提供Ga-68标记的双膦酸盐作为用于骨成像的正电子发射断层扫描（PET）示踪剂。初步人体研究表明，[Ga-68] Ga-HBED-CC-BP（[Ga-68]Ga-P15-041）与PET/计算机断层扫描（CT）联合使用显示在已知骨病变中蓄积，从血液和软组织中快速清除，并能够提供高对比度图像。描述了一种简单有效的冻干P15-041试剂盒制剂，用于在环境温度下快速生产具有优异放射化学纯度（RCP）的[Ga-68]Ga-P15-041，而无需纯化。结果表明，临床剂量的[Ga-68]Ga-P15-041可在几分钟内手动制备，纯度极佳（> 90%），且易于满足剂量放行标准。当在癌症患者中评价[Ga-68]Ga-P15-041时，显像剂清楚地显示在多个病变中的蓄积。结论：[Ga-68]Ga-P15-041是一种具有良好临床应用前景的骨显像剂。
One of the commonly performed studies in nuclear medicine are bone scans with [Tc-99m]Tc-methylene diphosphonate (MDP) for detecting various bone lesions, including cancer metastasis. The recent emergence of commercially available Ge-68/Ga-68 radionuclide generators makes it possible to provide Ga-68-labelled bisphosphonates as positron emission tomography (PET) tracers for bone imaging. Preliminary human studies suggested that [Ga-68] Ga-HBED-CC-BP ([Ga-68]Ga-P15-041) in conjunction with PET/computed tomography (CT) showed accumulation in known bone lesions, fast clearance from blood and soft tissue, and an ability to provide high contrast images. A simple and efficient lyophilized P15-041 kit formulation for the rapid production of [Ga-68]Ga-P15-041 with excellent radiochemical purity (RCP) under ambient temperature without the need for purification is described. It is demonstrated that clinical doses of [Ga-68]Ga-P15-041 can be prepared manually within minutes with an excellent purity (> 90%) and readily meet the dose release criteria. When [Ga-68]Ga-P15-041 was evaluated in a patient with cancer, the imaging agent clearly showed accumulations in multiple lesions. In conclusion, [Ga-68]Ga-P15-041, prepared by a lyophilized kit, might be an excellent bone imaging agent for widespread clinical application.