Abstract
The optimization of DOTA-NHS-ester conjugation to Rituximab using different Ab:DOTA molar ratios (1:10, 1:20, 1:50 and 1:100) was studied. High radiochemical yield, in vitro stability and immunoreactive fraction were obtained for the Rituximab conjugated at 1:50 molar ratio, resulting in the incorporation of an average number of 4.9 ± 1.1 DOTA per Rituximab molecule. Labeling with 177Lu was performed in high specific activity with great in vitro stability. Biodistribution in healthy and xenographed mice showed tumor uptake and high in vivo stability as evidenced by low uptake in bone. The properties of 177Lu-DOTA-Rituximab prepared from DOTA-NHS-ester suggest the potential for the application of the 177Lu-labeled antibody in preliminary clinical studies.
Keywords: Anti-CD-20, DOTA-NHS-ester, immunoconjugation, Non-Hodgking‘s Limphoma, radioimmunotherapy, Rituximab.
Current Radiopharmaceuticals
Title:Development and biological studies of 177Lu-DOTA-rituximab for the treatment of Non-Hodgkin’s lymphoma
Volume: 9 Issue: 1
Author(s): Adriana V.F. Massicano, Priscilla B. Pujatti, Lais F. Alcarde, Miriam F. Suzuki, Patrick J. Spencer and Elaine B. Araújo
Affiliation:
Keywords: Anti-CD-20, DOTA-NHS-ester, immunoconjugation, Non-Hodgking‘s Limphoma, radioimmunotherapy, Rituximab.
Abstract: The optimization of DOTA-NHS-ester conjugation to Rituximab using different Ab:DOTA molar ratios (1:10, 1:20, 1:50 and 1:100) was studied. High radiochemical yield, in vitro stability and immunoreactive fraction were obtained for the Rituximab conjugated at 1:50 molar ratio, resulting in the incorporation of an average number of 4.9 ± 1.1 DOTA per Rituximab molecule. Labeling with 177Lu was performed in high specific activity with great in vitro stability. Biodistribution in healthy and xenographed mice showed tumor uptake and high in vivo stability as evidenced by low uptake in bone. The properties of 177Lu-DOTA-Rituximab prepared from DOTA-NHS-ester suggest the potential for the application of the 177Lu-labeled antibody in preliminary clinical studies.
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Cite this article as:
Massicano V.F. Adriana, Pujatti B. Priscilla, Alcarde F. Lais, Suzuki F. Miriam, Spencer J. Patrick and Araújo B. Elaine, Development and biological studies of 177Lu-DOTA-rituximab for the treatment of Non-Hodgkin’s lymphoma, Current Radiopharmaceuticals 2016; 9 (1) . https://dx.doi.org/10.2174/1874471008666150313103849
DOI https://dx.doi.org/10.2174/1874471008666150313103849 |
Print ISSN 1874-4710 |
Publisher Name Bentham Science Publisher |
Online ISSN 1874-4729 |
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