1. 90Y-DOTA-Nimotuzumab: Synthesis of a Promising β- Radiopharmaceutical
- Author
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Scotognella, Teresa, Maccora, Daria, Bruno, Isabella, Chinol, Marco, Castagnola, Massimo, Collamati, Francesco, Mancini-Terraciano, Carlo, Morganti, Silvio, Bocci, Valerio, Camillocci, Elena Solfaroli, Rotili, Dante, Cartoni, Antonella, Fratoddi, Ilaria, Marini, Federica, Venditti, Iole, Faccini, Riccardo, and Giordano, Alessandro
- Abstract
Background: Nimotuzumab is a humanized anti-epidermal growth factor receptor(EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimedto label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate(
90 Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of anew radio-guided surgery approach. Methods: The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumabwas conjugated with a 50-fold excess of DOTA and then labelled with 90Y3+. The90 Y-DOTA-nimotuzumabpreparation was optimized considering several parameters such as pH, temperature and reactionvolume. Moreover, the90 Y-DOTA-nimotuzumab stability was evaluated in human plasma. Results: The radioimmunoconjugate90 Y-DOTA-nimotuzumab was obtained with a radiochemicalpurity 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 of90 Y-DOTA-nimotuzumabjoined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugateas a potential diagnostic radiopharmaceutical for β- radio-guided surgery.- Published
- 2022
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