90Y-DOTA-Nimotuzumab: Synthesis of a Promising β Radiopharmaceutical

(E-pub Ahead of Print)

Author(s): 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

Journal Name: Current Radiopharmaceuticals


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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.

Keywords: 90Y-DOTA-nimotuzumab, radio-guided surgery, molecular probe technique, radiopharmaceutical, monoclonal antibody

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Article Details

Published on: 04 January, 2021
(E-pub Ahead of Print)
DOI: 10.2174/1874471013999210104220031
Price: $95

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