Development and biological studies of ¹⁷⁷Lu-DOTA-rituximab for the treatment of Non-Hodgkin’s lymphoma

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.

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