Drug intelligence / Profile preview

birelentinib + rituximab + cyclophosphamide + doxorubicin + vincristine + prednisone

Development stage
Phase 3
Lead developer
Dizal Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

birelentinib + rituximab + cyclophosphamide + doxorubicin + vincristine + prednisone is an investigational chemoimmunotherapy regimen combining the novel LYN/BTK dual inhibitor birelentinib (DZD8586) with standard R-CHOP (rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone). Developed by Dizal, this combination is being evaluated as a first-line treatment for patients with newly diagnosed diffuse large B-cell lymphoma (DLBCL) in the Phase 2/3 TAI-SHAN19 trial (NCT07712588). Birelentinib is designed to penetrate the blood-brain barrier and inhibit both BTK-dependent and BTK-independent B-cell receptor (BCR) signaling pathways by targeting LYN and BTK, potentially overcoming resistance mechanisms seen with other BTK inhibitors. The addition of birelentinib to the standard R-CHOP backbone aims to improve efficacy in both germinal center B-cell (GCB) and non-GCB subtypes of DLBCL.

Other names
DZD8586 + R-CHOPDZD8586 + rituximab + cyclophosphamide + doxorubicin + vincristine + prednisoneDZD8586 plus R-CHOPDZD-8586 plus R-CHOPDZD 8586 plus R-CHOPbirelentinib + R-CHOPbirelentinib plus R-CHOP
02

Targets

CD20 (B-lymphocyte antigen CD20)DNATOP2A (DNA topoisomerase II)TOP2B (DNA topoisomerase II beta)GR (Glucocorticoid receptor)TUBB (Tubulin (alpha and beta subunits))BTK (Bruton tyrosine kinase)LYN (LYN proto-oncogene, Src family tyrosine kinase)

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