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bexobrutideg + rituximab
- 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 + rituximab (bexobrutideg + rituximab) is an investigational combination regimen being evaluated for the treatment of B-cell malignancies, including chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL). The combination consists of bexobrutideg (NX-5948), an orally bioavailable, brain-penetrant small-molecule targeted protein degrader (PROTAC) of Bruton's tyrosine kinase (BTK), and rituximab, a chimeric monoclonal antibody targeting CD20. Bexobrutideg induces the ubiquitination and subsequent proteasomal degradation of both wild-type and mutant forms of BTK via the cereblon (CRBN) E3 ligase complex, thereby overcoming resistance to conventional BTK inhibitors. Rituximab binds to CD20 on B cells, inducing cell death through antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC), and apoptosis. Together, the combination aims to provide synergistic anti-tumor activity by targeting B-cell receptor signaling and inducing direct B-cell depletion.
- Other names
- NX-5948 + rituximabrituximab + bexobrutidegrituximab + NX-5948
02
Targets
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