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

15 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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