Synthesis, Preclinical Validation, Dosimetry, and Toxicity of 68Ga-NOTA-Anti-HER2 Nanobodies for iPET Imaging of HER2 Receptor Expression in Cancer

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Synthesis, Preclinical Validation, Dosimetry, and Toxicity of 68Ga-NOTA-Anti-HER2 Nanobodies for iPET Imaging of HER2 Receptor Expression in Cancer. / Xavier, Catarina; Vaneycken, Ilse; D'huyvetter, Matthias; Heemskerk, Johannes; Keyaerts, Marleen; Vincke, Cécile; Devoogdt, Nick; Muyldermans, Serge; Lahoutte, Tony; Caveliers, Vicky; Aerts, An (Peer reviewer); Impens, Nathalie (Peer reviewer); Baatout, Sarah (Peer reviewer).

In: Journal of Nuclear Medicine, Vol. 54, No. 5, 13.05.2013, p. 776-784.

Research output: Contribution to journalArticle

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Xavier, C, Vaneycken, I, D'huyvetter, M, Heemskerk, J, Keyaerts, M, Vincke, C, Devoogdt, N, Muyldermans, S, Lahoutte, T, Caveliers, V, Aerts, A, Impens, N & Baatout, S 2013, 'Synthesis, Preclinical Validation, Dosimetry, and Toxicity of 68Ga-NOTA-Anti-HER2 Nanobodies for iPET Imaging of HER2 Receptor Expression in Cancer' Journal of Nuclear Medicine, vol 54, no. 5, pp. 776-784. DOI: 10.2967/jnumed.112.111021

Vancouver

Xavier C, Vaneycken I, D'huyvetter M, Heemskerk J, Keyaerts M, Vincke C et al. Synthesis, Preclinical Validation, Dosimetry, and Toxicity of 68Ga-NOTA-Anti-HER2 Nanobodies for iPET Imaging of HER2 Receptor Expression in Cancer. Journal of Nuclear Medicine. 2013 May 13;54(5):776-784. Available from, DOI: 10.2967/jnumed.112.111021

Author

Xavier, Catarina; Vaneycken, Ilse; D'huyvetter, Matthias; Heemskerk, Johannes; Keyaerts, Marleen; Vincke, Cécile; Devoogdt, Nick; Muyldermans, Serge; Lahoutte, Tony; Caveliers, Vicky; Aerts, An (Peer reviewer); Impens, Nathalie (Peer reviewer); Baatout, Sarah (Peer reviewer) / Synthesis, Preclinical Validation, Dosimetry, and Toxicity of 68Ga-NOTA-Anti-HER2 Nanobodies for iPET Imaging of HER2 Receptor Expression in Cancer.

In: Journal of Nuclear Medicine, Vol. 54, No. 5, 13.05.2013, p. 776-784.

Research output: Contribution to journalArticle

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@article{6d91004bf9cb4d0fb79c79a33c4bec83,
title = "Synthesis, Preclinical Validation, Dosimetry, and Toxicity of 68Ga-NOTA-Anti-HER2 Nanobodies for iPET Imaging of HER2 Receptor Expression in Cancer",
keywords = "HER2, breast cancer, nanobody, iPET",
author = "Catarina Xavier and Ilse Vaneycken and Matthias D'huyvetter and Johannes Heemskerk and Marleen Keyaerts and Cécile Vincke and Nick Devoogdt and Serge Muyldermans and Tony Lahoutte and Vicky Caveliers and An Aerts and Nathalie Impens and Sarah Baatout",
note = "Score=10",
year = "2013",
month = "5",
doi = "10.2967/jnumed.112.111021",
volume = "54",
pages = "776--784",
journal = "Journal of Nuclear Medicine",
issn = "0161-5505",
publisher = "SNMMI - Society of Nuclear Medicine and Molecular Imaging",
number = "5",

}

RIS - Download

TY - JOUR

T1 - Synthesis, Preclinical Validation, Dosimetry, and Toxicity of 68Ga-NOTA-Anti-HER2 Nanobodies for iPET Imaging of HER2 Receptor Expression in Cancer

AU - Xavier,Catarina

AU - Vaneycken,Ilse

AU - D'huyvetter,Matthias

AU - Heemskerk,Johannes

AU - Keyaerts,Marleen

AU - Vincke,Cécile

AU - Devoogdt,Nick

AU - Muyldermans,Serge

AU - Lahoutte,Tony

AU - Caveliers,Vicky

A2 - Aerts,An

A2 - Impens,Nathalie

A2 - Baatout,Sarah

N1 - Score=10

PY - 2013/5/13

Y1 - 2013/5/13

N2 - Nanobodies are the smallest fully functional antigen-binding antibody fragments possessing ideal properties as probes for molecular imaging. In this study we labeled the anti–human epidermal growth factor receptor type 2 (HER2) Nanobody with 68Ga via a 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) derivative and assessed its use for HER2 iPET imaging. Methods: The 2Rs15dHis6 Nanobody and the lead optimized current-good-manufacturing-practice grade analog 2Rs15d were conjugated with S-2-(4-isothiocyanatobenzyl)-1,4,7- triazacyclononane-1,4,7-triacetic acid (p-SCN-Bn-NOTA) to enable fast and efficient 68Ga labeling. Biodistribution and PET/CT studies were performed on HER2-positive and -negative tumor xenografts. The effect of injected mass on biodistribution was evaluated. The biodistribution data were extrapolated to calculate radiation dose estimates for the adult female using OLINDA software. A single-dose extended-toxicity study for NOTA- 2Rs15d was performed on healthy mice up to a dose of 10 mg/kg.

AB - Nanobodies are the smallest fully functional antigen-binding antibody fragments possessing ideal properties as probes for molecular imaging. In this study we labeled the anti–human epidermal growth factor receptor type 2 (HER2) Nanobody with 68Ga via a 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA) derivative and assessed its use for HER2 iPET imaging. Methods: The 2Rs15dHis6 Nanobody and the lead optimized current-good-manufacturing-practice grade analog 2Rs15d were conjugated with S-2-(4-isothiocyanatobenzyl)-1,4,7- triazacyclononane-1,4,7-triacetic acid (p-SCN-Bn-NOTA) to enable fast and efficient 68Ga labeling. Biodistribution and PET/CT studies were performed on HER2-positive and -negative tumor xenografts. The effect of injected mass on biodistribution was evaluated. The biodistribution data were extrapolated to calculate radiation dose estimates for the adult female using OLINDA software. A single-dose extended-toxicity study for NOTA- 2Rs15d was performed on healthy mice up to a dose of 10 mg/kg.

KW - HER2

KW - breast cancer

KW - nanobody

KW - iPET

UR - http://ecm.sckcen.be/OTCS/llisapi.dll/open/ezp_128827

UR - http://knowledgecentre.sckcen.be/so2/bibref/10210

U2 - 10.2967/jnumed.112.111021

DO - 10.2967/jnumed.112.111021

M3 - Article

VL - 54

SP - 776

EP - 784

JO - Journal of Nuclear Medicine

T2 - Journal of Nuclear Medicine

JF - Journal of Nuclear Medicine

SN - 0161-5505

IS - 5

ER -

ID: 258653