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lenalidomide + zanubrutinib
- Development stage
- Unknown
- Lead developer
- BeOne Medicines
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Lenalidomide + zanubrutinib is a combination therapy being evaluated by Henan Cancer Hospital for the treatment of primary and secondary central nervous system lymphoma (CNSL). Lenalidomide is an immunomodulatory agent that binds to cereblon (CRBN), part of the cullin-4 ring E3 ubiquitin ligase complex, leading to the ubiquitination and degradation of Ikaros (IKZF1) and Aiolos (IKZF3) transcription factors. Zanubrutinib is a small molecule, next-generation inhibitor of Bruton's tyrosine kinase (BTK) that forms a covalent bond with the enzyme to inhibit B-cell receptor (BCR) signaling. In clinical trials, this combination is often administered alongside rituximab as part of the ZR2 regimen, followed by a maintenance phase using either lenalidomide or zanubrutinib alone. The regimen is designed to provide a chemotherapy-free option for patients with CNS lymphoma, potentially reducing the severe complications associated with standard high-dose methotrexate-based treatments.
- Brand names
- RevlimidBrukinsa
- Other names
- lenalidomide and zanubrutinibzanubrutinib plus lenalidomideZR2 regimenZR-2 regimenZR 2 regimen
02
Targets
BTK (Bruton tyrosine kinase)CRBN (Cereblon)
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