Development and biological studies of sup(177)Lu-DOTA-rituximab for the treatment of non-hodgkin's lymphoma
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2016
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Current Radiopharmaceuticals
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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.
Citation
MASSICANO, ADRIANA V.F.; PUJATTI, PRISCILLA B.; ALCARDE, LAIS F.; SUZUKI, MIRIAM F.; SPENCER, PATRICK J.; ARAUJO, ELAINE B. Development and biological studies of sup(177)Lu-DOTA-rituximab for the treatment of non-hodgkin's lymphoma. Current Radiopharmaceuticals, v. 9, p. 54-63, 2016. DOI: 10.2174/1874471008666150313103849. Disponível em: http://repositorio.ipen.br/handle/123456789/25807. Acesso em: 17 Mar 2025.
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