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Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer.

Trastuzumab deruxtecan (1 pM-10 nM; 5 days) inhibits the growth of HER2‐positive KPL‐4 cells, with an IC₅₀ of 109.7 pM.
Trastuzumab deruxtecan (10 nM; 5 days) shows bystander killing effects in HER2‐negative MDA‐MB‐468 cells.

Trastuzumab deruxtecan (3 mg/kg; a single i.v.) shows antitumor activity against not only HER2‐positive tumors but also HER2‐negative tumors under the co‐inoculated condition.
Trastuzumab deruxtecan (10 mg/kg; i.v. on days 0 and 7) inhibits the tumor growth in in EMT6-hHER2 syngeneic mouse model.

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