Trastuzumab duocarmazine ((vic)-Trastuzumab duocarmazine) is an ADC targeting HER2, cleaved by histone B within tumor cells for selective targeting, exhibiting antitumor activity and applicable in cancer research, particularly for uterine and ovarian sarcomas [1].

Trastuzumab duocarmazine (SYD985) displayed cytotoxic activity against both HER2-negative and HER2-positive cell lines at concentrations ranging from 0.0001 to 100 μg/mL over a 24-hour period. It was seven times more potent against HER2/NEU 3+ cell lines, with an IC50 value of 0.013 μg/mL, compared to T-DM1, which had an IC50 value of 0.096 μg/mL. Notably, in HER2/NEU 1+ cells, the potency of SYD985 was 54 times higher than that of T-DM1 [1].

Trastuzumab duocarmazine (SYD985) administered intravenously at doses of 3 mg/kg or 10 mg/kg significantly inhibited tumor growth and prolonged survival in mice, demonstrating potent in vivo antitumor activity [1].

Human

Monoclonal