Drug intelligence / Profile preview

zanubrutinib + rituximab + lenalidomide

Development stage
Unknown
Lead developer
The First Affiliated Hospital of Wenzhou Medical University
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

The ZR2 regimen is a chemotherapy-free combination therapy consisting of zanubrutinib, rituximab, and lenalidomide. It is being investigated by the First Affiliated Hospital of Wenzhou Medical University for the treatment of newly diagnosed diffuse large B-cell lymphoma (DLBCL), specifically targeting elderly patients (aged 75 and older) who are considered unfit or frail for standard R-CHOP chemotherapy. Zanubrutinib is a potent, irreversible small-molecule inhibitor of Bruton's tyrosine kinase (BTK) that disrupts chronic B-cell receptor signaling. Rituximab is a chimeric monoclonal antibody targeting the CD20 antigen on B-lymphocytes, inducing cell death through immune-mediated mechanisms. Lenalidomide is an immunomodulatory agent that binds to the Cereblon E3 ubiquitin ligase complex, leading to the degradation of transcription factors like Ikaros and Aiolos and enhancing T-cell and NK-cell activity. This triplet combination aims to synergistically target genetic alterations and the tumor microenvironment in older DLBCL patients.

Other names
Zanubrutinib, Lenalidomide and RituximabZR2 regimenZR-2 regimenZR 2 regimen
02

Targets

CD20 (B-lymphocyte antigen CD20)CRBN (Cereblon)BTK (Bruton tyrosine kinase)

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