90Y-DOTA-nimotuzumab: Synthesis of a Promising β⁻ radiopharmaceutical

Author:

Scotognella Teresa1ORCID,Maccora Daria2,Bruno Isabella1,Chinol Marco3,Castagnola Massimo4,Collamati Francesco5,Mancini-Terraciano Carlo6,Morganti Silvio5,Bocci Valerio5,Camillocci Elena Solfaroli6,Rotili Dante7,Cartoni Antonella8,Fratoddi Ilaria8,Marini Federica9,Venditti Iole10,Faccini Riccardo5,Giordano Alessandro1

Affiliation:

1. Unit of Nuclear Medicine, Fondazione Policlinico Universitario A. Gemelli IRCCS, Roma, Italy

2. nstitute of Nuclear Medicine, Università Cattolica del Sacro Cuore, Roma;, Italy

3. Europeo di Oncologia, MilanoUnit of Nuclear Medicine, Istituto Europeo di Oncologia, Milano;, Italy

4. Laboratorio di Proteomica e Metabonomica – IRCCS Fondazione Santa Lucia;, Italy

5. Istituto Nazionale di Fisica Nucleare, Roma;, Italy

6. Department of Physics, Università Sapienza, Roma;, Italy

7. Department of Chemistry and Technologies of Drugs, “Sapienza” University of Rome, 00185 Rome,, Italy

8. Department of Chemistry, “Sapienza” University of Rome, 00185 Rome,, Italy

9. Institute of Biochemistry and Clinical Biochemistry, Università Cattolica del Sacro Cuore, Rome, 00168,, Italy

10. Department of Sciences, Università di Roma Tre, Roma,, Italy

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 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 90Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the 90Y-DOTA-nimotuzumab stability was evaluated in human plasma. Results: The radioimmunoconjugate 90Y-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 of 90Y-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.

Publisher

Bentham Science Publishers Ltd.

Subject

Pharmacology,Radiology Nuclear Medicine and imaging

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