Disitamab vedotin (RC-48) is a newly developed antibody-active molecule conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2), consisting of hertuzumab coupled to monomethyl auristatin E (MMAE) via a cleavable linker. Disitamab vedotin showed anti-tumor and anti-proliferative activities in gastric cancer cells with different HER-2 expression levels and inhibited the expression of HER-2 protein in gastric cancer cells.

OE19 cells:0.038 µg/mL, JIMT-1 cells:0.05 µg/mL, UACC-812 cells:0.012 µg/mL, EFM-192A cells:0.033 µg/mL, RN87 cells:0.239 µg/mL, N87 cells:0.028 µg/mL, BT-474 cells:0.033 µg/mL, SKBR3 cells:0.007 µg/mL

METHODS: Disitamab vedotin (RC-48) (0, 100, 500 ng/mL, 48 and 72 hours) treated E0771-hHER2 cells to determine cell viability and evaluate its effect on a breast cancer cell line lacking hHER2 expression (E0771 WT) Off-target effects.
RESULTS: E0771-hHER2 cell viability was measured in vitro, and the IC50 value was 90 ng/mL; Disitamab vedotin significantly reduced E0771-hHER2 cell viability. [3]

METHODS: Disitamab vedotin (RC-48) (10 mg/kg, intravenous injection) was used to treat PD-1 mice transplanted with E0771-hHER2 cells, and tumor growth in the mice was observed.
RESULTS: The average tumor volume of the disitamab vedotin-treated group on day 9 was 44.82±78.90 mm3; disitamab vedotin showed better anti-tumor effects. The anti-tumor effect of disitamab vedotin in this model mainly depends on the payload delivered by the anti-hHER2 antibody into the tumor. [3]