Drug intelligence / Profile preview

lenalidomide + zanubrutinib

Development stage
Phase 2
Lead developer
BeiGene
Modality
Small Molecules
Administration
Oral
01

Overview

Lenalidomide + zanubrutinib is a combination therapy being investigated for various B-cell malignancies. Zanubrutinib is a second-generation Bruton's tyrosine kinase (BTK) inhibitor that forms a covalent bond with cysteine 481 in the ATP-binding pocket of BTK, blocking B-cell receptor signaling and inhibiting malignant B-cell proliferation. Lenalidomide is an immunomodulatory drug with direct anti-tumor activity and immune-enhancing effects. The combination leverages complementary mechanisms to potentially improve outcomes in lymphoid cancers. Clinical trials are evaluating this combination with or without rituximab (as ZR² regimen) for diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), and other B-cell malignancies.

Other names
ZR²ZR2ZR-2ZR 2
02

Targets

BTK (Bruton tyrosine kinase)CRBN (Cereblon)

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