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Year : 2013  |  Volume : 9  |  Issue : 2  |  Page : 199-204

Optimization of 90 Y-antiCD20 preparation for radioimmunotherapy

1 Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2 Department of Engineering and Technical, Science and Research Branch, Islamic Azad University, Tehran, 14778-93855, Iran
3 Radiopharmaceutical Research and Development Lab (RRDL), Nuclear Science and Technology Research Institute (NSTRI), Tehran, 14155-1339, Iran

Correspondence Address:
Amir Reza Jalilian
Radiopharmaceutical Research and Development Lab (RRDL), Nuclear ­Science and Technology Research Institute (NSTRI), Tehran, 14155-1339
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Source of Support: None, Conflict of Interest: None

DOI: 10.4103/0973-1482.113350

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Context: The advent of monoclonal antibodies such as Rituximab, in recent years, has brought about decisive progress in the treatment of aggressive and indolent non-Hodgkin's lymphoma. Aims: A further tried and tested improvement to the unmodified antibody has been its coupling to the beta-emitters Y-90. The optimization of 90 Y-antiCD20 radioimmunoconjugate production and quality control methods for future clinical studies in the country was targeted in this work. Materials and Methods: The antibody was labeled with 90 Y-yttrium chloride (185 MBq) after conjugation with freshly prepared ccDTPA. Y-90 chloride was obtained by thermal neutron flux (4 × 10 13 n/cm 2 /s) of a natural Y 2 O 3 sample, dissolved in acidic media. Radiolabeling was completed in 24 h by the addition of DTPA-Rituximab conjugate at room temperature. Statistical Analysis Used: All values were expressed as mean ± standard deviation (mean ± SD), and the data were compared using Student's t-test. Statistical significance was defined as P < 0.05. Results: Radiochemical purity of 96% was obtained by using ITLC method for the final radioimmunoconjugate (specific activity = 440-480 MBq/mg). The final isotonic 90 Y-Rituximab complex was checked by gel electrophoresis for protein integrity retention. Biodistribution studies in normal rats were carried out to determine the radioimmunoconjugate distribution up to 72 h. Conclusion: The results showed that 90 Y-DTPA-Rituximab could be considered for further evaluation in animals and possibly in humans as a radiopharmaceutical for use in radioimmunotherapy against non-Hodgkin's lymphomas. Because of the importance of developing anti-lymphoma B agents in nuclear medicine for country use, an optimized radiolabeling method has been introduced.

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