Drug intelligence / Profile preview

brentuximab vedotin

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Brentuximab vedotin is a CD30-directed antibody-drug conjugate (ADC) used primarily in the treatment of various lymphomas. It consists of a chimeric IgG1 monoclonal antibody (brentuximab/cAC10) targeting the cell surface protein CD30, which is commonly expressed on malignant cells in classical Hodgkin lymphoma and systemic anaplastic large cell lymphoma. The antibody is covalently linked via a protease-cleavable valine-citrulline linker to monomethyl auristatin E (MMAE), a potent microtubule-disrupting agent. Upon binding to CD30-expressing tumor cells, the ADC is internalized and MMAE is released inside the cell by lysosomal enzymes. MMAE then binds tubulin and disrupts microtubules, leading to cell cycle arrest and apoptotic death of cancer cells[3][4][5]. Brentuximab vedotin was developed by Seagen (formerly Seattle Genetics) and initially approved in 2011 for relapsed or refractory Hodgkin lymphoma and systemic anaplastic large cell lymphoma[3][5]. Its indications have since expanded to include frontline therapy for advanced classical Hodgkin lymphoma in adults and high-risk pediatric patients when combined with chemotherapy[2][6][9].

Brand names
Adcetris
Other names
brentuximab vedotinSGN-35SGN35SGN 35cAC10-vcMMAEcAC-10-vcMMAEcAC 10-vcMMAE
02

Targets

CD30 (CD30 antigen)TUBB (Tubulin (alpha and beta subunits))

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