Drug intelligence / Profile preview

mocetinostat + brentuximab vedotin

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules, Peptide-Drug Conjugates → Peptide Conjugates → Peptides, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Oral, Intravenous
01

Overview

Mocetinostat + brentuximab vedotin is an investigational combination therapy for cancer, particularly in relapsed or refractory Hodgkin lymphoma. Mocetinostat is a small molecule histone deacetylase (HDAC) inhibitor that modulates gene expression and induces apoptosis in cancer cells. Brentuximab vedotin is an antibody-drug conjugate consisting of an anti-CD30 monoclonal antibody linked to the microtubule-disrupting agent monomethyl auristatin E (MMAE). Brentuximab vedotin binds to CD30-expressing tumor cells, is internalized, and releases MMAE intracellularly to disrupt microtubules, causing cell cycle arrest and apoptosis[2][3][6]. The combination aims to enhance antitumor activity by targeting both epigenetic regulation (via HDAC inhibition) and direct cytotoxicity against CD30-positive lymphoma cells.

02

Targets

TUBB (Tubulin (alpha and beta subunits))CD30 (CD30 antigen)HDAC8 (Histone Deacetylase 8)

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