Trastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate functioning as a HER2-targeted topoisomerase I inhibitor, with targeting capability and antitumor activity, employed in research on HER2-positive breast cancer and gastric cancer.

Axl (KPL-4 cells):109.7 pM

Methods: In HER2-positive (SK-BR-3, HCC1419), low-expressing (ZR-75-1, SNU-601), and negative (MDA-MB-231) cells, treatment with Trastuzumab deruxtecan (0–500 ng/mL) was performed for 120 hours.
Results: Clonogenic assays showed HER2-dependent differences in IC50 values, with HER2-positive cells being the most sensitive. Western blot confirmed inhibition of HER2 downstream signaling, and annexin V assays demonstrated induction of apoptosis. [1]

Methods: Tumor-bearing mice were randomly grouped and received intravenous injection of Trastuzumab deruxtecan (10 mg/kg, dissolved in 0.9% NaCl) or vehicle control on days 1, 7, and 21.
Results: The treatment group significantly delayed tumor progression and prolonged survival (median survival 37.5 days vs. 16.5 days, p = 0.0032).[2]
Methods: In a cynomolgus monkey toxicity model, intravenous injection was administered once every 3 weeks for 6 weeks or 3 months, at doses of 10, 30, 78.8 mg/kg (6 weeks) or 3, 10, 30 mg/kg (3 months), with histidine buffer as the vehicle.
Results: Doses of 30 mg/kg and above induced interstitial pneumonia, manifested as diffuse lymphocytic infiltration and mild fibrosis.[3]

CHO

Human

Immobilized Human ERBB2/HER2/CD340, His Tag at 2 μg/mL (30 μL/well) can bind Trastuzumab deruxtecan. The EC50 is 0.01391 μg/mL.

Monoclonal

DXd