Preparation, biological characterization and preliminary human imaging studies of 68Ga-DOTA-IBA

作者：Yingwei Wang, Qixin Wang, Zan Chen, Jian Yang, Hanxiang Liu, Dengsai Peng, Lei Lei, Lin Liu, Li Wang, Naiguo Xing, Lin Qiu, Yue Feng, Yue Chen · 发表于：Frontiers in Oncology · 年份：2022 · DOI：10.3389/fonc.2022.1027792 · 被引用次数：40 · 研究领域：Radiopharmaceutical Chemistry and Applications、Medical Imaging Techniques and Applications、Bone health and treatments

Purpose In this study, DOTA-IBA was radiolabeled with 68 Ga and we determined the optimum labelling conditions and assessed the biological properties of 68 Ga-DOTA-IBA. We investigated the biodistribution of 68 Ga-DOTA-IBA in normal animals and undertook PET/CT imaging in humans. Finally, we explored the feasibility 68 Ga-DOTA-IBA as a bone imaging agent and demonstrated its potential for the therapeutic release of 177 Lu/ 225 Ac-DOTA-IBA. Methods The controlled variables method was used to assess the impact of variables on the radiochemical purity of 68 Ga-DOTA-IBA. The biological properties of 68 Ga-DOTA-IBA were investigated. 68 Ga-DOTA-IBA micro-PET/CT imaging was performed on animals. Volunteers were recruited for 68 Ga-DOTA-IBA imaging and data were compared to 99m Tc-MDP imaging studies to calculate the target to non-target ratio (T/NT) of the lesions. Results The prepared 68 Ga-DOTA-IBA had a radiochemical purity of >97% and demonstrated good biological properties with a good safety profile in normal mice. PET/CT imaging of the animals showed rapid blood clearance with high contrast between the bone and stroma. Human imaging showed that 68 Ga-DOTA-IBA could detect more lesions compared to 99m Tc-MDP and had a higher targeted to untargeted ratio. Conclusions 68 Ga-DOTA-IBA is an osteophilic radiopharmaceutical that can be synthesized using a simple labelling method. 68 Ga-DOTA-IBA has high radiochemical purity and is stable in vitro stability. It is rapidly clea...