Drug intelligence / Profile preview

chidamide + rituximab + cyclophosphamide + doxorubicin + vincristine + prednisone + orelabrutinib

Development stage
Phase 2
Lead developer
Innocare
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

CR-CHOP + orelabrutinib is an experimental combination regimen being investigated for the treatment of newly diagnosed double-expression diffuse large B-cell lymphoma (DEL DLBCL). The regimen builds upon the standard R-CHOP immunochemotherapy backbone (rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone) by adding two targeted agents: chidamide (tucidinostat), a selective histone deacetylase (HDAC) inhibitor, and orelabrutinib, a highly selective, irreversible Bruton's tyrosine kinase (BTK) inhibitor. This combination is designed to simultaneously target epigenetic dysregulation and B-cell receptor signaling pathways, which are frequently co-opted in high-risk DLBCL subtypes. The regimen is currently being evaluated in a Phase II molecularly stratified trial led by Ruijin Hospital to assess its efficacy and safety in patients with MYC and BCL2 double-expression.

Brand names
Orelabru
Other names
Chidamide + R-CHOP + orelabrutinibtucidinostat + R-CHOP + orelabrutinibCR-CHOP-O
02

Targets

BTK (Bruton tyrosine kinase)CD20 (B-lymphocyte antigen CD20)DNAGR (Glucocorticoid receptor)HDAC1 (Histone Deacetylase 1)HDAC10 (Histone Deacetylase 10)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)TOP2A (DNA topoisomerase II)TUBB (Tubulin (alpha and beta subunits))

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