Lutetuim-177 labeled Rituximab: Opened gateway to better radioimmunotherapy

Smilkov, Katarina and Gjorgieva Ackova, Darinka and Janevik-Ivanovska, Emilija and Chinol, Marco and Carollo, Angela and Gjorgoski, Icko (2015) Lutetuim-177 labeled Rituximab: Opened gateway to better radioimmunotherapy. In: 4th Balkan Congress of Nuclear Medicine, 03-06 Sept 2015, Ohrid, R. Macedonia.


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The beginning of the new century brought approval of two monoclonal antibodies for therapy of Non Hodgkin's Lymphoma (NHL), Bexxar® and Zevalin®, and opened the gateway to the research in targeted therapy of, mostly haematological malignanices. Since then, the research has been directed toward improvement in three principal, but interdependent factors: the antibody, the radionuclide, and the target tumor/host. Among the most researched anti-CD 20 monoclonal antibodies is rituximab, and among the radionuclides, Y-90, In-111, Cu-64, Sm-153, and Lu-177–labeled antibodies have been described or are under development. The aim of our research was to develop a new lyophilized kit, ready-to label with Lu-177, with a potential to be used in diagnostic and therapeutic purposes. In our experiments, we used rituximab, purified from a commercial preparation, Mabthera®, that was conjugated using p-SCN-Bn-DOTA, p-SCN-Bn-DTPA and 1B4M-DTPA as chelating agents. The lyophilized kit was prepared in three-day lyophilization protocol. The radiolabeling of the lyophilized kits was performed after reconstitution in 0.9% NaCl, in the presence of acetate ions at pH 7.0 with Lutetium-177, SA 555 GBq/mg, at RT. The RCP was determined using size-exclusion (SE-HPLC). The results showed preserved antibody structure and suitability for successful radiolabelling with over 95% RCP in all three radioimmunoconjugates, encouraging further evaluation experiments. Regarding the results obtained, further experiments will be performed in order to demonstrate their biological and pharmacological properties.

Item Type: Conference or Workshop Item (Speech)
Subjects: Natural sciences > Biological sciences
Natural sciences > Chemical sciences
Medical and Health Sciences > Health biotechnology
Medical and Health Sciences > Health sciences
Medical and Health Sciences > Other medical sciences
Divisions: Faculty of Medical Science
Depositing User: Katarina Smilkov
Date Deposited: 25 Jan 2016 12:53
Last Modified: 25 Jan 2016 12:53

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