ImmunoPET imaging of EpCAM in solid tumours with nanobody tracers: a preclinical study.

Purpose: Epithelial cell adhesion molecule (EpCAM) is a potential therapeutic target and anchoring molecule for circulating and disseminated tumour cells (CTC/DTC) in liquid biopsy. In this study, we aimed to construct EpCAM-specific immuno-positron emission tomography (immunoPET) imaging probes and...

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Publicado en:European Journal of Nuclear Medicine & Molecular Imaging Vol. 52; no. 2; pp. 388 - 401
Autores principales: Xu, Dongsheng, Zhang, You, Huang, Wei, Pan, Xinbing, An, Shuxian, Wang, Cheng, Huang, Gang, Liu, Jianjun, Wei, Weijun
Formato: Journal Article
Publicado: Springer Nature Jan2025
Acceso en línea:Ver este registro en EBSCOhost
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      dt: Jan2025
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      pub: Springer Nature
      place: New York, New York
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        179525074
        10.1007/s00259-024-06910-8
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        atl: ImmunoPET imaging of EpCAM in solid tumours with nanobody tracers: a preclinical study.
      aug:
        au:
          Xu, Dongsheng
          Zhang, You
          Huang, Wei
          Pan, Xinbing
          An, Shuxian
          Wang, Cheng
          Huang, Gang
          Liu, Jianjun
          Wei, Weijun
        affil: https://ror.org/0220qvk04 Department of Nuclear Medicine, Institute of Clinical Nuclear Medicine, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, 200127, Shanghai, China
      sug:
      ab: Purpose: Epithelial cell adhesion molecule (EpCAM) is a potential therapeutic target and anchoring molecule for circulating and disseminated tumour cells (CTC/DTC) in liquid biopsy. In this study, we aimed to construct EpCAM-specific immuno-positron emission tomography (immunoPET) imaging probes and assess the diagnostic abilities in preclinical cancer models. Methods: By engineering six single-domain antibodies (e.g., EPCD1 − 6) targeting EpCAM of different binding properties and labelling with 68Ga (T1/2 = 1.1 h) and 18F (T1/2 = 110 min), we developed a series of EpCAM-targeted immunoPET imaging probes. The probes' pharmacokinetics and diagnostic accuracies were investigated in cell-derived human colorectal (LS174T) and esophageal cancer (OE19) tumour models. Results: Based on in vitro binding affinities and in vivo pharmacokinetics of the first three tracers ([68Ga]Ga-NOTA-EPCD1, [68Ga]Ga-NOTA-EPCD2, and [68Ga]Ga-NOTA-EPCD3), we selected [68Ga]Ga-NOTA-EPCD3 for tumour imaging which showed an average tumour uptake of 2.06 ± 0.124%ID/g (n = 3) in LS174T cell-derived tumour model. Development and characterisation of [18F]AIF-RESCA-EPCD3 showed comparable tumour uptake of 1.73 ± 0.0471%ID/g (n = 3) in the same tumour model. Further validation of [68Ga]Ga-NOTA-EPCD3 in OE19 cell-derived tumour model showed an average tumour uptake of 4.27 ± 1.16%ID/g and liver uptake of 13.5 ± 1.30%ID/g (n = 3). Near-infrared fluorescence imaging with Cy7-EPCD3 confirmed the in vivo pharmacokinetics and relatively high liver accumulation. We further synthesized another three 18F-labeled nanobody tracers ([18F]AIF-RESCA-EPCD4, [18F]AIF-RESCA-EPCD5, and [18F]AIF-RESCA-EPCD6) and found that [18F]AIF-RESCA-EPCD6 had the best pharmacokinetics with low background. [18F]AIF-RESCA-EPCD6 showed explicit uptake in the subcutaneously inoculated OE19 tumour model with an average uptake of 4.70 ± 0.26%ID/g (n = 3). In comparison, the corresponding tumour uptake (0.17 ± 0.25%ID/g, n = 3) in the EPCD6 blocking group was substantially lower (P < 0.001), indicating the targeting specificity of the tracer. Conclusions: We developed a series of 68Ga/18F-labeled nanobody tracers targeting human EpCAM. ImmunoPET imaging with [18F]AIF-RESCA-EPCD6 may facilitate better use of EpCAM-targeted therapeutics by noninvasively displaying the target's expression dynamics.
      pubtype: Academic Journal
      doctype: Journal Article
      ougenre: Article
    language: English
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