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bortezomib + rituximab + cyclophosphamide + prednisone

Development stage
Unknown
Lead developer
Millennium Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous, Oral, Subcutaneous
01

Overview

This is a **four-drug combination regimen** composed of **bortezomib** (a reversible proteasome inhibitor), **rituximab** (a chimeric monoclonal antibody targeting CD20 on B cells), **cyclophosphamide** (an alkylating agent causing DNA crosslinking), and **prednisone** (a synthetic glucocorticoid with anti-inflammatory and immunosuppressive effects). Such regimens are investigated primarily in B-cell non-Hodgkin lymphoma, including diffuse large B-cell lymphoma (DLBCL) and indolent NHL, as an analog to R-CHOP regimens, sometimes termed "VR-CAP" when doxorubicin is omitted or "B-R-CHP" when vincristine is omitted. The goal is to improve efficacy over standard regimens by incorporating the proteasome inhibitor bortezomib, which induces apoptosis especially in malignant B cells resistant to other agents. Multiple phase II studies have evaluated this combination for increased response rates and survival in DLBCL and follicular lymphoma[1][3].

02

Targets

GR (Glucocorticoid receptor)CD20 (B-lymphocyte antigen CD20)PSMB5 (Proteasome subunit beta Type-5)DNA

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