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venetoclax + trastuzumab emtansine
- Development stage
- Discontinued
- Lead developer
- Roche
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
A combination of **venetoclax**, a selective, oral small-molecule inhibitor of the antiapoptotic protein BCL-2, and **trastuzumab emtansine** (T-DM1, Kadcyla), an antibody–drug conjugate comprising trastuzumab linked to the cytotoxic agent DM1. Venetoclax promotes cancer cell apoptosis by inhibiting BCL-2, disrupting survival signals in cancer cells, while trastuzumab emtansine targets HER2-overexpressing cells, delivering DM1 to induce cell cycle arrest and apoptosis. This combination was investigated for previously treated HER2-positive locally advanced or metastatic breast cancer, to potentially improve efficacy in this population[2][3][9].
- Brand names
- VenclextaKadcyla
- Other names
- venetoclax plus trastuzumab emtansinevenetoclax + T-DM1venetoclax + Kadcyla
02
Targets
BCL-2 (BCL-2 family)TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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