Gallium-68-Labeled Anti-HER2 Single-Chain Fv Fragment

Development and In Vivo Monitoring of HER2 Expression

Masashi Ueda, Hayato Hisada, Takashi Temma, Yoichi Shimizu, Hiroyuki Kimura, Masahiro Ono, Yuji Nakamoto, Kaori Togashi, Hideo Saji

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Purpose: We aimed to develop a gallium-68 (Ga-68)-labeled single-chain variable fragment (scFv) targeting the human epidermal growth factor receptor 2 (HER2) to rapidly and noninvasively evaluate the status of HER2 expression.Procedures: Anti-HER2 scFv was labeled with Ga-68 by using deferoxamine (Df) as a bifunctional chelate. Biodistribution of [68Ga]Df-anti-HER2 scFv was examined with tumor-bearing mice and positron emission tomography (PET) imaging was performed. The changes in HER2 expression after anti-HER2 therapy were monitored by PET imaging.Results: [68Ga]Df-anti-HER2 scFv was obtained with high radiochemical yield after only a 5-min reaction at room temperature. The probe showed high accumulation in HER2-positive xenografts and the intratumoral distribution of radioactivity coincided with HER2-positive regions. Furthermore, [68Ga]Df-anti-HER2 scFv helped visualize HER2-positive xenografts and monitor the changes in HER2 expression after anti-HER2 therapy.Conclusion: [68Ga]Df-anti-HER2 scFv could be a promising probe to evaluate HER2 status by in vivo PET imaging, unless trastuzumab is prescribed as part of the therapy.

Original languageEnglish
Pages (from-to)102-110
Number of pages9
JournalMolecular Imaging and Biology
Volume17
Issue number1
DOIs
Publication statusPublished - 2014

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Immunoglobulin Variable Region
Single-Chain Antibodies
Gallium
Deferoxamine
Positron-Emission Tomography
human ERBB2 protein
Heterografts

Keywords

  • 17-DMAG
  • Gallium-68
  • Human epidermal growth factor receptor 2(HER2)
  • Positron emission tomography (PET)
  • Single-chain Fv Fragment (scFv)
  • Therapy

ASJC Scopus subject areas

  • Cancer Research
  • Oncology
  • Radiology Nuclear Medicine and imaging
  • Medicine(all)

Cite this

Gallium-68-Labeled Anti-HER2 Single-Chain Fv Fragment : Development and In Vivo Monitoring of HER2 Expression. / Ueda, Masashi; Hisada, Hayato; Temma, Takashi; Shimizu, Yoichi; Kimura, Hiroyuki; Ono, Masahiro; Nakamoto, Yuji; Togashi, Kaori; Saji, Hideo.

In: Molecular Imaging and Biology, Vol. 17, No. 1, 2014, p. 102-110.

Research output: Contribution to journalArticle

Ueda, M, Hisada, H, Temma, T, Shimizu, Y, Kimura, H, Ono, M, Nakamoto, Y, Togashi, K & Saji, H 2014, 'Gallium-68-Labeled Anti-HER2 Single-Chain Fv Fragment: Development and In Vivo Monitoring of HER2 Expression', Molecular Imaging and Biology, vol. 17, no. 1, pp. 102-110. https://doi.org/10.1007/s11307-014-0769-5
Ueda, Masashi ; Hisada, Hayato ; Temma, Takashi ; Shimizu, Yoichi ; Kimura, Hiroyuki ; Ono, Masahiro ; Nakamoto, Yuji ; Togashi, Kaori ; Saji, Hideo. / Gallium-68-Labeled Anti-HER2 Single-Chain Fv Fragment : Development and In Vivo Monitoring of HER2 Expression. In: Molecular Imaging and Biology. 2014 ; Vol. 17, No. 1. pp. 102-110.
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AB - Purpose: We aimed to develop a gallium-68 (Ga-68)-labeled single-chain variable fragment (scFv) targeting the human epidermal growth factor receptor 2 (HER2) to rapidly and noninvasively evaluate the status of HER2 expression.Procedures: Anti-HER2 scFv was labeled with Ga-68 by using deferoxamine (Df) as a bifunctional chelate. Biodistribution of [68Ga]Df-anti-HER2 scFv was examined with tumor-bearing mice and positron emission tomography (PET) imaging was performed. The changes in HER2 expression after anti-HER2 therapy were monitored by PET imaging.Results: [68Ga]Df-anti-HER2 scFv was obtained with high radiochemical yield after only a 5-min reaction at room temperature. The probe showed high accumulation in HER2-positive xenografts and the intratumoral distribution of radioactivity coincided with HER2-positive regions. Furthermore, [68Ga]Df-anti-HER2 scFv helped visualize HER2-positive xenografts and monitor the changes in HER2 expression after anti-HER2 therapy.Conclusion: [68Ga]Df-anti-HER2 scFv could be a promising probe to evaluate HER2 status by in vivo PET imaging, unless trastuzumab is prescribed as part of the therapy.

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