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trastuzumab deruxtecan + pyrotinib
- Development stage
- Preclinical
- Lead developer
- Daiichi Sankyo
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous, Oral
01
Overview
A combination of trastuzumab deruxtecan (Enhertu), an antibody-drug conjugate, and pyrotinib, an irreversible pan-ErbB receptor tyrosine kinase inhibitor. Both drugs target HER2-positive cancers through different mechanisms. Trastuzumab deruxtecan combines the HER2-targeting monoclonal antibody trastuzumab with the topoisomerase I inhibitor deruxtecan, while pyrotinib irreversibly binds to ATP binding sites in HER1, HER2, and HER4 intracellular segments.
- Brand names
- Enhertu + pyrotinib
- Other names
- fam-trastuzumab deruxtecan-nxki + pyrotinib
02
Targets
TOP1 (DNA Topoisomerase I)ERBB4 (Erb-b2 receptor tyrosine kinase 4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)
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