Chlorambucil Conjugation Enhances the Potency of Rituximab: Synthesis and Evaluation of the Novel [¹⁷⁷Lu]Lu-Labeled Rituximab-Chlorambucil Conjugate toward Therapy of Non-Hodgkin’s Lymphoma

Naveen Kumar; Sunil Kumar Suman; Mohini Guleria; Soumi Kolay; Jeyachitra Amirdhanayagam; Avik Chakraborty; Sutapa Rakshit; Archana Mukherjee; Tapas Das

doi:10.1021/acs.jmedchem.4c01954

January 14, 2025Journal of Medicinal Chemistry

Chlorambucil Conjugation Enhances the Potency of Rituximab: Synthesis and Evaluation of the Novel [¹⁷⁷Lu]Lu-Labeled Rituximab-Chlorambucil Conjugate toward Therapy of Non-Hodgkin’s Lymphoma

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Key Points

This research aims to evaluate the effectiveness of a chlorambucil-rituximab conjugate for treating non-Hodgkin’s lymphoma.
Synthesis of chlorambucil-rituximab conjugate with Lu-177 labeling.
Ex vivo experiments assessing tumor accumulation and organ uptake after co-injection with cold Rituximab.
SPECT-CT imaging used to analyze biodistribution and tumor targeting effectiveness.
Administration of Lu-177 labeled Rituximab resulted in 25.25 ± 0.8% cell death at 83.99 MBq/mg.
Co-injection with cold Rituximab improved tumor accumulation and reduced nontarget organ uptake.
SPECT-CT imaging confirmed enhanced tumor-targeting and biodistribution of the conjugate.

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Implication

Evaluates chlorambucil-rituximab conjugate effectiveness in non-Hodgkin’s lymphoma, suggesting improved outcomes.

Abstract

Lu]Lu-labeled-Rituximab (83.99 MBq/mg) (25.25 ± 0.8% cell death) when administered at similar radioactivity doses. Ex vivo experiments indicated that coinjecting cold Rituximab with the radiolabeled formulations significantly improved tumor accumulation and reduced nontarget organ uptake. SPECT-CT imaging results supported these findings, further confirming the enhanced tumor-targeting and biodistribution of the radiolabeled ADC.

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Kumar et al. (2025) studied this question.

synapsesocial.com/papers/6a082b369a6c4ba6e6108242 https://doi.org/10.1021/acs.jmedchem.4c01954

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Chlorambucil Conjugation Enhances the Potency of Rituximab: Synthesis and Evaluation of the Novel [¹⁷⁷Lu]Lu-Labeled Rituximab-Chlorambucil Conjugate toward Therapy of Non-Hodgkin’s Lymphoma

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Chlorambucil Conjugation Enhances the Potency of Rituximab: Synthesis and Evaluation of the Novel [¹⁷⁷Lu]Lu-Labeled Rituximab-Chlorambucil Conjugate toward Therapy of Non-Hodgkin’s Lymphoma

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