90Y-DOTA-nimotuzumab: Synthesis of a Promising β⁻ radiopharmaceutical

Teresa Scotognella; Daria Maccora; Isabella Bruno; Marco Chinol; Massimo Castagnola; Francesco Collamati; Carlo Mancini-Terraciano; Silvio Morganti; Valerio Bocci; Elena Solfaroli Camillocci; Dante Rotili; Antonella Cartoni; Ilaria Fratoddi; Federica Marini; Iole Venditti; Riccardo Faccini; Alessandro Giordano

doi:10.2174/1874471013999210104220031

90Y-DOTA-nimotuzumab: Synthesis of a Promising β⁻ radiopharmaceutical

Teresa Scotognella, Daria Maccora, Isabella Bruno, Marco Chinol, Massimo Castagnola, Francesco Collamati, Carlo Mancini-Terraciano, Silvio Morganti, Valerio Bocci, Elena Solfaroli Camillocci, Dante Rotili, Antonella Cartoni, Ilaria Fratoddi, Federica Marini, Iole Venditti, Riccardo Faccini, Alessandro Giordano

Research output: Contribution to journal › Article › peer-review

Abstract

BACKGROUND: Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (90Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.

METHODS: The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50 fold excess of DOTA and then labelled with 90Y3+. The 90Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the 90Y-DOTA-nimotuzumab stability was evaluated in human plasma.

RESULTS: The radioimmunoconjugate 90Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.

CONCLUSIONS: The optimized conditions for a mild and easy preparation of 90Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.

Original language	English
Journal	Current Radiopharmaceuticals
DOIs	https://doi.org/10.2174/1874471013999210104220031
Publication status	E-pub ahead of print - Jan 4 2021

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Scotognella, T., Maccora, D., Bruno, I., Chinol, M., Castagnola, M., Collamati, F., Mancini-Terraciano, C., Morganti, S., Bocci, V., Camillocci, E. S., Rotili, D., Cartoni, A., Fratoddi, I., Marini, F., Venditti, I., Faccini, R., & Giordano, A. (2021). 90Y-DOTA-nimotuzumab: Synthesis of a Promising β⁻ radiopharmaceutical. Current Radiopharmaceuticals. https://doi.org/10.2174/1874471013999210104220031

Scotognella, T, Maccora, D, Bruno, I, Chinol, M, Castagnola, M, Collamati, F, Mancini-Terraciano, C, Morganti, S, Bocci, V, Camillocci, ES, Rotili, D, Cartoni, A, Fratoddi, I, Marini, F, Venditti, I, Faccini, R & Giordano, A 2021, '90Y-DOTA-nimotuzumab: Synthesis of a Promising β⁻ radiopharmaceutical', Current Radiopharmaceuticals. https://doi.org/10.2174/1874471013999210104220031

@article{f47be78ec96a4f0883f6e4161803b957,

title = "90Y-DOTA-nimotuzumab: Synthesis of a Promising β⁻ radiopharmaceutical",

abstract = "BACKGROUND: Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (90Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.METHODS: The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50 fold excess of DOTA and then labelled with 90Y3+. The 90Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the 90Y-DOTA-nimotuzumab stability was evaluated in human plasma.RESULTS: The radioimmunoconjugate 90Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.CONCLUSIONS: The optimized conditions for a mild and easy preparation of 90Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.",

author = "Teresa Scotognella and Daria Maccora and Isabella Bruno and Marco Chinol and Massimo Castagnola and Francesco Collamati and Carlo Mancini-Terraciano and Silvio Morganti and Valerio Bocci and Camillocci, {Elena Solfaroli} and Dante Rotili and Antonella Cartoni and Ilaria Fratoddi and Federica Marini and Iole Venditti and Riccardo Faccini and Alessandro Giordano",

note = "Copyright{\textcopyright} Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.",

year = "2021",

month = jan,

day = "4",

doi = "10.2174/1874471013999210104220031",

language = "English",

journal = "Current Radiopharmaceuticals",

issn = "1874-4710",

publisher = "Bentham Science Publishers B.V.",

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TY - JOUR

T1 - 90Y-DOTA-nimotuzumab

T2 - Synthesis of a Promising β⁻ radiopharmaceutical

AU - Scotognella, Teresa

AU - Maccora, Daria

AU - Bruno, Isabella

AU - Chinol, Marco

AU - Castagnola, Massimo

AU - Collamati, Francesco

AU - Mancini-Terraciano, Carlo

AU - Morganti, Silvio

AU - Bocci, Valerio

AU - Camillocci, Elena Solfaroli

AU - Rotili, Dante

AU - Cartoni, Antonella

AU - Fratoddi, Ilaria

AU - Marini, Federica

AU - Venditti, Iole

AU - Faccini, Riccardo

AU - Giordano, Alessandro

PY - 2021/1/4

Y1 - 2021/1/4

N2 - BACKGROUND: Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (90Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.METHODS: The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50 fold excess of DOTA and then labelled with 90Y3+. The 90Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the 90Y-DOTA-nimotuzumab stability was evaluated in human plasma.RESULTS: The radioimmunoconjugate 90Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.CONCLUSIONS: The optimized conditions for a mild and easy preparation of 90Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.

AB - BACKGROUND: Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (90Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.METHODS: The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50 fold excess of DOTA and then labelled with 90Y3+. The 90Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the 90Y-DOTA-nimotuzumab stability was evaluated in human plasma.RESULTS: The radioimmunoconjugate 90Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.CONCLUSIONS: The optimized conditions for a mild and easy preparation of 90Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.

U2 - 10.2174/1874471013999210104220031

DO - 10.2174/1874471013999210104220031

M3 - Article

C2 - 33397277

SN - 1874-4710

JO - Current Radiopharmaceuticals

JF - Current Radiopharmaceuticals

ER -

90Y-DOTA-nimotuzumab: Synthesis of a Promising β⁻ radiopharmaceutical

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