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., et al. (2022). 90 Y-DOTA-Nimotuzumab: Synthesis of a Promising β− Radiopharmaceutical. CURRENT RADIOPHARMACEUTICALS, 15(1), 32-39 [10.2174/1874471013999210104220031].
90 Y-DOTA-Nimotuzumab: Synthesis of a Promising β− Radiopharmaceutical
Rotili D.;Venditti I.;
2022-01-01
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
