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

Authors :: 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
Source :: Current radiopharmaceuticals [Curr Radiopharm] 2022; Vol. 15 (1), pp. 32-39.
Publication Year :: 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 ( <superscript>90</superscript> Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.<br />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 <superscript>90</superscript> Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the <superscript>90</superscript> Y-DOTA-nimotuzumab stability was evaluated in human plasma.<br />Results: The radioimmunoconjugate <superscript>90</superscript> Y-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.<br />Conclusions: The optimized conditions for a mild and easy preparation of <superscript>90</superscript> Y-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.<br /> (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)