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68Ga-DOTA-Neratinib: A novel small-molecule PET tracer for breast cancer imaging

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机构： [1]Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, China [2]Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, China [3]Nuclear Medicine Institute of Southwest Medical University, Luzhou, China [4]Nuclear Medicine Oncology Department, 92493 Hospital of PLA, Huludao, China

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Current DOTA-based 68Ga-labeled small-molecule probes targeting HER2 often suffer from limited tumor-specific uptake. To overcome this limitation, we selected Neratinib, a second-generation pan-HER tyrosine kinase inhibitor, and successfully developed a novel PET imaging agent, 68Ga-DOTA-Neratinib. The probe demonstrated high radiochemical yield, excellent in vitro and in vivo stability, and strong binding affinity for the HER2 receptor. Cell uptake assays confirmed specific accumulation in HER2-positive cell lines: uptake in BT-474 and SK-BR-3 cells at 2 h post-incubation was 7.55 ± 1.10 % and 8.18 ± 0.56 %, respectively, significantly higher than that in HER2-negative MCF-7 cells (4.71 ± 0.79 %, P < 0.05). Moreover, micro-PET/CT imaging in HER2-positive tumor-bearing mice showed enhanced tumor uptake and prolonged intratumoral retention of the tracer, though some background blood activity was also observed. These findings suggest that 68Ga-DOTA-Neratinib is a promising small-molecule PET probe for the noninvasive imaging of HER2-positive breast cancer.Copyright © 2025. Published by Elsevier Inc.

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出版当年[2025]版：

大类 | 2 区医学

小类 | 1 区有机化学 2 区生化与分子生物学

最新[2025]版：

大类 | 2 区医学

小类 | 1 区有机化学 2 区生化与分子生物学

第一作者：

第一作者机构： [1]Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, China [2]Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, China [3]Nuclear Medicine Institute of Southwest Medical University, Luzhou, China

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通讯机构： [1]Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, China [2]Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, China [3]Nuclear Medicine Institute of Southwest Medical University, Luzhou, China [*1]Department of Nuclear Medicine, The Affiliated Hospital of Southwest Medical University, Luzhou, China.

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