Drug intelligence / Profile preview

rituximab + cyclophosphamide + doxorubicin + vincristine + prednisone + orelabrutinib

Development stage
Unknown
Lead developer
InnoCare Pharma
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

R-CHOP + orelabrutinib is a combination chemoimmunotherapy regimen investigated for the treatment of B-cell malignancies, particularly diffuse large B-cell lymphoma (DLBCL). The regimen combines the standard-of-care R-CHOP (rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone) with orelabrutinib (ICP-022), a highly selective, irreversible second-generation Bruton's tyrosine kinase (BTK) inhibitor developed by InnoCare Pharma. Orelabrutinib provides sustained BTK occupancy and high selectivity, minimizing off-target effects compared to first-generation inhibitors. The combination is specifically targeted at the MCD genetic subtype of DLBCL, which is characterized by MYD88 and CD79B mutations and is highly dependent on B-cell receptor (BCR) signaling. Clinical evaluation includes the Phase 3 BELIEVE-01 trial comparing this combination against R-CHOP plus placebo.

Brand names
Yikaini
Other names
R-CHOP + ICP-022R-CHOP plus orelabrutinibR-CHOP + orelabrutinib
02

Targets

CD20 (B-lymphocyte antigen CD20)TOP2A (DNA topoisomerase II)C1Q (Complement C1q)GR (Glucocorticoid receptor)DNAFcγR (Low affinity immunoglobulin gamma Fc region receptor II-c)TUBB (Tubulin (alpha and beta subunits))BTK (Bruton tyrosine kinase)

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