Drug intelligence / Profile preview

brentuximab vedotin + rituximab + etoposide + cyclophosphamide + doxorubicin + dacarbazine + dexamethasone

Development stage
Preclinical
Lead developer
Takeda
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

This is a multi-agent combination chemotherapy regimen composed of seven drugs: - **Brentuximab vedotin** is an antibody-drug conjugate targeting CD30, delivering the cytotoxic agent monomethyl auristatin E to malignant cells. - **Rituximab** is a monoclonal antibody targeting CD20 on B lymphocytes, leading to cell lysis. - **Etoposide** is a topoisomerase II inhibitor that induces DNA strand breaks and apoptosis in rapidly dividing cells. - **Cyclophosphamide** is an alkylating agent that crosslinks DNA, inhibiting cell replication. - **Doxorubicin** (also known as hydroxydaunorubicin) intercalates into DNA and inhibits topoisomerase II, causing cytotoxicity. - **Dacarbazine** acts as an alkylating agent after metabolic activation, damaging DNA in cancer cells. - **Dexamethasone** is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive properties. This combination has been investigated for the treatment of aggressive lymphomas such as relapsed or refractory large B-cell lymphoma (LBCL), including diffuse large B-cell lymphoma (DLBCL), particularly in patients who are not eligible for stem cell transplantation or CAR T-cell therapy. The regimen leverages multiple mechanisms—targeted immunotherapy, cytotoxic chemotherapy, and steroid modulation—to maximize antitumor efficacy.

02

Targets

CD20 (B-lymphocyte antigen CD20)CD30 (CD30 antigen)TOP2A (DNA topoisomerase II)GR (Glucocorticoid receptor)TUBB (Tubulin (alpha and beta subunits))

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