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trastuzumab deruxtecan
- Development stage
- Approved
- Lead developer
- Daiichi Sankyo
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Trastuzumab deruxtecan is an antibody-drug conjugate used to treat certain types of unresectable or metastatic HER2-positive and HER2-low breast cancer, as well as HER2-positive gastric or gastroesophageal junction adenocarcinoma and other solid tumors. It consists of a humanized anti-HER2 IgG1 monoclonal antibody (trastuzumab) covalently linked via a cleavable peptide linker to the topoisomerase I inhibitor deruxtecan (DXd). The drug binds to the HER2 receptor on tumor cells, is internalized, and releases DXd inside the cell through enzymatic cleavage. This results in targeted DNA damage and apoptosis in cancer cells. Trastuzumab deruxtecan was developed by Daiichi Sankyo in collaboration with AstraZeneca and was first approved by the FDA in 2019[1][3][8].
- Brand names
- Enhertu
- Other names
- fam-trastuzumab deruxtecan-nxkiT-DXd
02
Targets
TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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