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 of90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50-fold excess of DOTA and then labelled with90Y3+. The90Y-DOTA-nimo-tuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the90Y-DOTA-nimotuzumab stability was evaluated in human plasma. Results: The radioimmunoconjugate90Y-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 of90Y-DOTA-nimo-tuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.
Scotognella, T., Maccora, D., Bruno, I., Chinol, M., Castagnola, M., Collamati, F., Mancini-Terraciano, C., Morganti, S., Bocci, V., Solfaroli Camillocci, E., Rotili, D., Cartoni, A., Fratoddi, I., Marini, F., Venditti, I., Faccini, R., Giordano, A., 90 Y-DOTA-Nimotuzumab: Synthesis of a Promising β− Radiopharmaceutical, <<CURRENT RADIOPHARMACEUTICALS>>, 2008; 15 (1): 32-39. [doi:10.2174/1874471013999210104220031] [http://hdl.handle.net/10807/210223]
90 Y-DOTA-Nimotuzumab: Synthesis of a Promising β− Radiopharmaceutical
Scotognella, Teresa;Maccora, Daria;Castagnola, Massimo;Giordano, Alessandro
2022
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 of90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50-fold excess of DOTA and then labelled with90Y3+. The90Y-DOTA-nimo-tuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the90Y-DOTA-nimotuzumab stability was evaluated in human plasma. Results: The radioimmunoconjugate90Y-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 of90Y-DOTA-nimo-tuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.
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