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zongertinib + trastuzumab deruxtecan
- Development stage
- Unknown
- Lead developer
- Boehringer Ingelheim
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
**Zongertinib + trastuzumab deruxtecan** is an investigational combination therapy studied for the treatment of advanced cancers with HER2 overexpression or mutation. **Zongertinib** (BI 1810631) is a selective, orally administered tyrosine kinase inhibitor (TKI) targeting **HER2** (human epidermal growth factor receptor 2), designed to spare EGFR and reduce off-target toxicities. **Trastuzumab deruxtecan** (T-DXd, Enhertu) is an antibody-drug conjugate (ADC) that delivers a cytotoxic topoisomerase I inhibitor payload directly to HER2-expressing cancer cells. Both drugs act via distinct mechanisms—zongertinib as a small-molecule inhibitor and trastuzumab deruxtecan as an ADC—converging on HER2-driven oncogenesis. The combination is being evaluated in the Beamion BCGC-1 trial for HER2+ metastatic breast cancer and gastrointestinal cancers, aiming to improve response rates and outcomes in previously treated patients[1][2].
- Other names
- fam-trastuzumab deruxtecan-nxki
02
Targets
TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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