Frontiers in Oncology (Dec 2022)
Preparation, biological characterization and preliminary human imaging studies of 68Ga-DOTA-IBA
- Yingwei Wang,
- Yingwei Wang,
- Yingwei Wang,
- Qixin Wang,
- Qixin Wang,
- Qixin Wang,
- Zan Chen,
- Jian Yang,
- Jian Yang,
- Jian Yang,
- Hanxiang Liu,
- Hanxiang Liu,
- Hanxiang Liu,
- Dengsai Peng,
- Dengsai Peng,
- Dengsai Peng,
- Lei Lei,
- Lei Lei,
- Lei Lei,
- Lin Liu,
- Lin Liu,
- Lin Liu,
- Li Wang,
- Li Wang,
- Li Wang,
- Naiguo Xing,
- Naiguo Xing,
- Naiguo Xing,
- Lin Qiu,
- Lin Qiu,
- Lin Qiu,
- Yue Feng,
- Yue Feng,
- Yue Feng,
- Yue Chen,
- Yue Chen,
- Yue Chen
Affiliations
- Yingwei Wang
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Yingwei Wang
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Yingwei Wang
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Qixin Wang
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Qixin Wang
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Qixin Wang
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Zan Chen
- Department of Orthopaedics, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Jian Yang
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Jian Yang
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Jian Yang
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Hanxiang Liu
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Hanxiang Liu
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Hanxiang Liu
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Dengsai Peng
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Dengsai Peng
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Dengsai Peng
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Lei Lei
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Lei Lei
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Lei Lei
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Lin Liu
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Lin Liu
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Lin Liu
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Li Wang
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Li Wang
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Li Wang
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Naiguo Xing
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Naiguo Xing
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Naiguo Xing
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Lin Qiu
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Lin Qiu
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Lin Qiu
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Yue Feng
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Yue Feng
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Yue Feng
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- Yue Chen
- Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan, China
- Yue Chen
- Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan, China
- Yue Chen
- Nuclear Medicine Institute of Southwest Medical University, Luzhou, Sichuan, China
- DOI
- https://doi.org/10.3389/fonc.2022.1027792
- Journal volume & issue
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Vol. 12
Abstract
PurposeIn this study, DOTA-IBA was radiolabeled with 68Ga and we determined the optimum labelling conditions and assessed the biological properties of 68Ga-DOTA-IBA. We investigated the biodistribution of 68Ga-DOTA-IBA in normal animals and undertook PET/CT imaging in humans. Finally, we explored the feasibility 68Ga-DOTA-IBA as a bone imaging agent and demonstrated its potential for the therapeutic release of 177Lu/225Ac-DOTA-IBA.MethodsThe controlled variables method was used to assess the impact of variables on the radiochemical purity of 68Ga-DOTA-IBA. The biological properties of 68Ga-DOTA-IBA were investigated.68Ga-DOTA-IBA micro-PET/CT imaging was performed on animals. Volunteers were recruited for 68Ga-DOTA-IBA imaging and data were compared to 99mTc-MDP imaging studies to calculate the target to non-target ratio (T/NT) of the lesions.ResultsThe prepared 68Ga-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 68Ga-DOTA-IBA could detect more lesions compared to 99mTc-MDP and had a higher targeted to untargeted ratio.Conclusions68Ga-DOTA-IBA is an osteophilic radiopharmaceutical that can be synthesized using a simple labelling method. 68Ga-DOTA-IBA has high radiochemical purity and is stable in vitro stability. It is rapidly cleared from the blood, has low toxicity and has strong targeting to the bone with long retention times. We also found that it is rapidly cleared in non-target tissues and has high contrast on whole-body bone imaging. 68Ga-DOTA-IBA PET/CT has potential as a novel bone imaging bone modality in patients with metastatic disease.
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