TY - JOUR
T1 - 90 Y-DOTA-Nimotuzumab: Synthesis of a Promising β− Radiopharmaceutical
AU - Scotognella, Teresa
AU - Maccora, Daria
AU - Bruno, Isabella
AU - Chinol, Marco
AU - Castagnola, Massimo
AU - Collamati, Francesco
AU - Mancini-Terraciano, Carlo
AU - Morganti, Silvio
AU - Bocci, Valerio
AU - Solfaroli Camillocci, Elena
AU - Rotili, Dante
AU - Cartoni, Antonella
AU - Fratoddi, Ilaria
AU - Marini, Federica
AU - Venditti, Iole
AU - Faccini, Riccardo
AU - Giordano, Alessandro
PY - 2022
Y1 - 2022
N2 - 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.
AB - 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.
KW - 90Y-DOTA-nimotuzumab
KW - Antibodies, Monoclonal
KW - Antibodies, Monoclonal, Humanized
KW - Antineoplastic Agents
KW - Heterocyclic Compounds
KW - Humans
KW - Immunoconjugates
KW - Organometallic Compounds
KW - Radiopharmaceuticals
KW - Yttrium Radioisotopes
KW - immunochemotherapy
KW - molecular probe technique
KW - monoclonal antibody
KW - radio-guided surgery
KW - radiopharmaceutical
KW - 90Y-DOTA-nimotuzumab
KW - Antibodies, Monoclonal
KW - Antibodies, Monoclonal, Humanized
KW - Antineoplastic Agents
KW - Heterocyclic Compounds
KW - Humans
KW - Immunoconjugates
KW - Organometallic Compounds
KW - Radiopharmaceuticals
KW - Yttrium Radioisotopes
KW - immunochemotherapy
KW - molecular probe technique
KW - monoclonal antibody
KW - radio-guided surgery
KW - radiopharmaceutical
UR - http://hdl.handle.net/10807/210223
U2 - 10.2174/1874471013999210104220031
DO - 10.2174/1874471013999210104220031
M3 - Article
SN - 1874-4710
VL - 15
SP - 32
EP - 39
JO - Current Radiopharmaceuticals
JF - Current Radiopharmaceuticals
ER -