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177lu-dota-rituximab

Development stage
Preclinical
Lead developer
University Hospital Basel
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

177Lu-DOTA-rituximab is a radiolabeled monoclonal antibody conjugate developed for radioimmunotherapy. It consists of rituximab, a chimeric anti-CD20 monoclonal antibody, covalently conjugated to a DOTA chelator, which is then labeled with the radionuclide lutetium-177 (177Lu). The DOTA chelator stabilizes the linkage, and the 177Lu delivers targeted beta radiation to CD20-positive B cells, providing cytotoxic effects especially exploited in the treatment of B-cell non-Hodgkin lymphoma, including relapsed or refractory subtypes. The preparation can utilize different forms of DOTA activation chemistry (e.g., SCN or NHS). The mechanism combines the immunologic targeting action of rituximab (binding CD20) with the localized emission of radiation via 177Lu, leading to increased tumor cell death both by direct antibody-mediated and radiation-induced effects. Preclinical and early clinical studies indicate good in vitro stability, preserved immunoreactivity, and in vivo antitumor activity. The product is experimental and used primarily in the research setting for lymphoma therapy[1][3][5].

Other names
177Lu-DOTA-rituximablutetium-177 DOTA-rituximablutetium177 DOTA-rituximablutetium 177 DOTA-rituximab177Lu-labeled DOTA-rituximab177Lu-anti-CD20-DOTA-rituximab
02

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