Development and clinical evaluation of [68Ga]Ga-NODAGA-ADAPT6 as a novel HER2-targeted PET radiotracer for breast cancer imaging and treatment monitoring.

Purpose: Accurate assessment of human epidermal growth factor receptor type 2 (HER2) expression is crucial for diagnosis, treatment planning, and monitoring of breast cancer patients. A 68Ga-labeled tracer based on the albumin-binding domain-derived affinity protein 6 (ADAPT6) was developed to evalu...

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Published in:European Journal of Nuclear Medicine & Molecular Imaging Vol. 52; no. 11; pp. 4078 - 4092
Main Authors: Tao, Weijing, Zhang, Jinglin, Meng, Xin, Han, Xuedong, Wang, Qiuhu, Lin, Yixiang, Cheng, Luyi, Liu, Minmin, Da, Dongzhu, Zhang, Huai, Fan, Junfu, Zhang, Lianmei, Liu, Shuangyue, Li, Shuo, Gao, Feng, Ren, Yi
Format: Journal Article
Published: Springer Nature Sep2025
Online Access:View this record in EBSCOhost
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      dt: Sep2025
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      pub: Springer Nature
      place: New York, New York
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        10.1007/s00259-025-07286-z
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        atl: Development and clinical evaluation of [68Ga]Ga-NODAGA-ADAPT6 as a novel HER2-targeted PET radiotracer for breast cancer imaging and treatment monitoring.
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        au:
          Tao, Weijing
          Zhang, Jinglin
          Meng, Xin
          Han, Xuedong
          Wang, Qiuhu
          Lin, Yixiang
          Cheng, Luyi
          Liu, Minmin
          Da, Dongzhu
          Zhang, Huai
          Fan, Junfu
          Zhang, Lianmei
          Liu, Shuangyue
          Li, Shuo
          Gao, Feng
          Ren, Yi
        affil: https://ror.org/00xpfw690 Department of Nuclear Medicine, The Affiliated Huaian No. 1 People's Hospital of Nanjing Medical University, No. 1 Huanghe West Road, 223300, Huai'an, Jiangsu, China
      sug:
      ab: Purpose: Accurate assessment of human epidermal growth factor receptor type 2 (HER2) expression is crucial for diagnosis, treatment planning, and monitoring of breast cancer patients. A 68Ga-labeled tracer based on the albumin-binding domain-derived affinity protein 6 (ADAPT6) was developed to evaluate HER2 expression in breast cancer. Methods: The gene encoding ADAPT6 was modified with N-terminal (GHEHEHEDANS) and C-terminal (GSSC) extensions to enhance its functionality. The precursor was synthesized, purified, and characterized, followed by radiolabeling with 68Ga to produce [68Ga]Ga-NODAGA-ADAPT6. In vivo metabolism and biodistribution studies were performed in HCC1954 (HER2-positive) and MDA-MB-468 (HER2-negative) tumor-bearing mice. Additionally, with ethical approval and informed consent, 22 breast cancer patients underwent [68Ga]Ga-NODAGA-ADAPT6 PET imaging to assess HER2 expression in primary and metastatic lesions. Results: The tracer was prepared with a radiochemical purity exceeding 99% and demonstrated high stability in vivo. Micro-PET/CT imaging revealed significant accumulation of the radiotracer in HCC1954 tumors, which was markedly reduced after HER2 blockade with trastuzumab. In contrast, MDA-MB-468 tumors showed minimal uptake. In the clinical study, [68Ga]Ga-NODAGA-ADAPT6 PET images displayed varying levels of radiotracer uptake in primary and metastatic lesions, which correlated well with the HER2 expression status determined by pathological analysis. Conclusion: [68Ga]Ga-NODAGA-ADAPT6 exhibited excellent pharmacokinetic properties and high specificity for HER2-expressing lesions in PET imaging. These findings highlight its potential as a promising tool for distinguishing different levels of HER2 expression in breast cancer, aiding in personalized treatment strategies.
      pubtype: Academic Journal
      doctype: Journal Article
      ougenre: Article
    language: English
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