Development and standardization of Rituximab-conjugates for labeling with Lutetium-177 and Yttrium-90

Janevik-Ivanovska, Emilija and Gjorgieva Ackova, Darinka and Smilkov, Katarina and Gjorgoski, Icko and Stafilov, Trajče and Makreski, Petre and Arsova-Sarafinovska, Zorica and Baloch, Lajos and Carollo, Angela and Signore, Alberto and Duatti, Adriano (2016) Development and standardization of Rituximab-conjugates for labeling with Lutetium-177 and Yttrium-90. Macedonian pharmaceutical bulletin, 62 (Supp). 537 -538. ISSN 1409 - 8695

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The main goal was to investigate chemical characterization of the immunoconjugates, labelled with “cold” non-radioactive isotopes of Lutetium and Yttrium in the same conditions as with radioactive Lutetium 177 and to show the chemical behaviour and toxicological properties.
After evaluation of all obtained results obtained we can conclude:
Three immunoconjugates were synthesized, using p-SCN-Bn-DOTA, p-SCN-Bn-DTPA and 1B4M-DTPA using the selected ration, 1 : 20,
Protocol for lyophilization was established, yielding lyophilizate with favourable physicochemical properties.
The non-radioactive labelling with Y and Lu showed preserved secondary structure in all three types of immunoconjugates, confirming their stability in conditions of freeze-drying and labelling.
During labelling with Lu-177 all three types of radioimmunoconjugates showed high radiochemical purity, over 95%, which was confirmed both in ITLC and SE-HPLC.
The selection of the most appropriate immunoconjugate kit suitable for labelling with Lu-177 or with Y-90 can be made after stability study of the formulation and completion of cell culture studies.

Item Type: Article
Subjects: Medical and Health Sciences > Basic medicine
Natural sciences > Biological sciences
Natural sciences > Chemical sciences
Divisions: Faculty of Medical Science
Depositing User: Zorica Arsova Sarafinovska
Date Deposited: 09 Jul 2020 07:21
Last Modified: 09 Jul 2020 07:21

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