Trastuzumab deruxtecan (Synonyms: DS-8201 (solution); DS-8201a (solution))

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[1][2].

Trastuzumab deruxtecan (1 pM-10 nM; 5 days) inhibits the growth of HER2‐positive KPL‐4 cells, with an IC50 of 109.7 pM[2].Trastuzumab deruxtecan (10 nM; 5 days) shows bystander killing effects in HER2‐negative MDA‐MB‐468 cells[2]. Cell Viability Assay[2] Cell Line: KPL‐4 and 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[2].Trastuzumab deruxtecan (10 mg/kg; i.v. on days 0 and 7) inhibits the tumor growth in in EMT6-hHER2 syngeneic mouse model[3]. Animal Model: Female BALB/c nude mice injected with NCI‐N87 and MDA‐MB‐468‐Luc cells[2]

[1]. Kotani D, et, al. Trastuzumab deruxtecan for the treatment of patients with HER2-positive gastric cancer. Ther Adv Med Oncol. 2021 Jan 7;13:1758835920986518. [2]. Ogitani Y, et, al. Bystander killing effect of DS-8201a, a novel anti-human epidermal growth factor receptor 2 antibody-drug conjugate, in tumors with human epidermal growth factor receptor 2 heterogeneity. Cancer Sci. 2016 Jul;107(7):1039-46. [3]. Iwata TN, et, al. [Fam-] trastuzumab deruxtecan (DS-8201a)-induced antitumor immunity is facilitated by the anti-CTLA-4 antibody in a mouse model. PLoS One. 2019 Oct 1;14(10):e0222280.