Trastuzumab deruxtecan (T-DXd) is an antibody-active molecule conjugate (ADC) with anticancer and antitumor activity, which is composed of a monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2) coupled to a topoisomerase I inhibitor (DXd). Trastuzumab deruxtecan has an improved effect on the treatment of HER2-positive breast cancer and gastric cancer.

Axl (KPL-4 cells):109.7 pM

METHODS: HER2-positive KPL-4 cells were treated with Trastuzumab deruxtecan (T-DXd) (1 pM-10 nM, 5 days) and cell viability was calculated.
RESULTS: Trastuzumab deruxtecan can inhibit the growth of HER2-positive KPL-4 cells with an IC50 value of 109.7 pM. [2]
METHODS: Trastuzumab deruxtecan (10 nM, 5 days) was used to treat co-cultured HER2-positive KPL-4 cells and HER2-negative MDA-MB-468 cells, and the number of viable cells was measured to determine whether it induced bystander killing.
RESULTS: Trastuzumab deruxtecan killed both KPL-4 and MDA-MB-468 cells. [2]

METHODS: Trastuzumab deruxtecan (T-DXd) (10 mg/kg, intravenous injection) was used to treat EMT6-hHER2 tumor-bearing mice, and the changes in tumors in the mice were observed.
RESULTS: Trastuzumab deruxtecan significantly inhibited tumor growth in EMT6-hHER2 tumor-bearing mice 18 days after treatment. [1]