Drug intelligence / Profile preview

bexobrutideg + obinutuzumab

Development stage
Unknown
Lead developer
Nurix Therapeutics
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

NX-5948 + obinutuzumab is an investigational drug combination consisting of bexobrutideg (NX-5948), an oral, brain-penetrant, highly selective small-molecule degrader of Bruton's tyrosine kinase (BTK), and obinutuzumab (Gazyva), an approved glycoengineered, type II anti-CD20 monoclonal antibody. Bexobrutideg functions as a proteolysis-targeting chimera (PROTAC) that recruits the cereblon (CRBN) E3 ubiquitin ligase complex to induce the ubiquitination and subsequent proteasomal degradation of both wild-type and mutated forms of BTK, thereby overcoming resistance to conventional BTK inhibitors. Obinutuzumab targets CD20 on B cells, inducing direct cell death and enhancing antibody-dependent cellular cytotoxicity (ADCC). The combination is being co-developed by Nurix Therapeutics and Roche and is currently in Phase 1b/2 clinical trials for the treatment of B-cell malignancies, including chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL).

Other names
NX-5948 + obinutuzumabbexobrutideg + obinutuzumabobinutuzumab + NX-5948obinutuzumab + bexobrutideg
02

Targets

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

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