Datopotamab deruxtecan (DS-1062) is a trophoblast cell surface antigen 2 (TROP2)-targeted antibody-drug conjugate (ADC) with antitumor activity. Datopotamab deruxtecan induces significant antibody-dependent cellular cytotoxicity in the presence of peripheral blood lymphocytes and inhibits tumor growth in xenograft models.

BxPC-3 cells (Trop2-expressing):74.6 ng/mL, HGSOC cells (TROP2-negative) viability:5.1 µM, CFPAC-1 cells (Trop2-expressing):706 ng/mL, TROP2-over expressing HGSOC cells viability:0.49 µM

Datopotamab deruxtecan specifically binds to TROP2. 100 μg/mL Datopotamab deruxtecan is internalized into the tumor cell and reaches the lysosome via the intracellular transport pathway and releases Deruxtecan. In vitro experiments Datopotamab deruxtecan caused DNA damage and triggered apoptosis in tumor cells expressing TROP2. [1]

Datopotamab deruxtecan exhibited significant antitumor activity in a variety of TROP2-expressing xenograft tumors, and 6 mg/kg Datopotamab deruxtecan treatment of a patient-derived xenograft (PDX) model of non-small-cell lung cancer (NSCLC) induced tumor regression. In addition, Datopotamab deruxtecan has an acceptable safety profile in rats and crab-eating monkeys. [1]

Human

Immobilized Human TROP2 Protein (His) at 2 μg/mL (30 μL/well) can bind Datopotamab deruxtecan. The EC50 is 0.006524 μg/mL.

Monoclonal

DXd