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ZN-1041 + trastuzumab deruxtecan
- Development stage
- Unknown
- Lead developer
- Roche
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
ZN-1041 + trastuzumab deruxtecan is a combination therapy consisting of ZN-1041, a blood-brain barrier (BBB) penetrable HER2 tyrosine kinase inhibitor (TKI), and trastuzumab deruxtecan (Enhertu), an antibody-drug conjugate. This combination is being investigated for the treatment of HER2-positive breast cancer with or without central nervous system (CNS) metastases. Preclinical studies have shown that the combination demonstrates significant improvement in intracranial tumor growth inhibition compared to trastuzumab deruxtecan alone. In clinical trials, the combination has shown promising efficacy in treatment-refractory settings, including in patients who previously progressed on trastuzumab deruxtecan and/or TKI therapy.
- Brand names
- Enhertu
- Other names
- trastuzumab deruxtecanDS-8201aDS8201aDS 8201a
02
Targets
TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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