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

Current Radiopharmaceuticals
Adriana V F MassicanoElaine B Araújo

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.

Citations

Apr 2, 2019·International Reviews of Immunology·Mahsa EskianNima Rezaei
Apr 8, 2020·Cancer Biotherapy & Radiopharmaceuticals·Wioletta WojdowskaPiotr Garnuszek
Jan 26, 2021·Bioorganic & Medicinal Chemistry·Ana Cláudia Camargo MirandaElaine Bortoleti de Araújo

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