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poziotinib + ado-trastuzumab emtansine
- Development stage
- Preclinical
- Lead developer
- Assertio
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
**poziotinib + ado-trastuzumab emtansine** is a combination investigational therapy for HER2-positive cancers. Poziotinib is an orally available, irreversible small molecule tyrosine kinase inhibitor targeting HER2 (ERBB2), EGFR (ERBB1), and HER4 (ERBB4) receptors. Ado-trastuzumab emtansine (T-DM1) is an antibody-drug conjugate composed of trastuzumab (a monoclonal antibody targeting HER2) linked to DM1 (a cytotoxic maytansine derivative) via a stable linker; it delivers targeted cytotoxic activity directly to HER2-overexpressing cells. This combination is proposed to provide dual HER2 blockade: poziotinib inhibits signaling through HER-family receptors, while ado-trastuzumab emtansine induces targeted cytotoxicity. The primary indication is treatment of advanced or metastatic HER2-positive breast cancer, particularly after progression on prior HER2-targeted therapies.
- Other names
- poziotinib + T-DM1poziotinib plus ado-trastuzumab emtansine
02
Targets
EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))ERBB4 (Erb-b2 receptor tyrosine kinase 4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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