Drug intelligence / Profile preview

ibrutinib + rituximab + cyclophosphamide + doxorubicin + vincristine + prednisone

Development stage
Phase 3
Lead developer
Janssen Research & Development
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

This is a **combination chemotherapy regimen** containing six active drugs: - **Ibrutinib** is a small molecule Bruton tyrosine kinase (BTK) inhibitor that blocks B-cell receptor signaling, leading to reduced proliferation and survival of malignant B cells. - **Rituximab** is a monoclonal antibody targeting CD20 on B lymphocytes, leading to cell lysis primarily by antibody-dependent cellular cytotoxicity, complement-dependent cytotoxicity, and apoptosis. - **Cyclophosphamide** is an alkylating agent that cross-links DNA, interfering with cell division and causing cell death. - **Doxorubicin** is an anthracycline antibiotic that intercalates DNA and inhibits topoisomerase II, disrupting replication and transcription. - **Vincristine** is a vinca alkaloid that inhibits microtubule formation in mitosis, thus disrupting cell division. - **Prednisone** is a synthetic glucocorticoid with anti-inflammatory and lympholytic effects. The combination is under investigation in certain B-cell malignancies, including variants of non-Hodgkin lymphomas, notably diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), and experimental settings for chronic lymphocytic leukemia (CLL). This regimen is a variant of the established R-CHOP protocol, adding ibrutinib for targeted BTK inhibition, and is sometimes referred to as IR-CHOP in trial settings.

Other names
IR-CHOP
02

Targets

BTK (Bruton tyrosine kinase)CD20 (B-lymphocyte antigen CD20)DNAGR (Glucocorticoid receptor)MicrotubuleTOP2A (DNA topoisomerase II)TUBB (Tubulin (alpha and beta subunits))

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