Glembatumumab vedotin binds to GPNMB on tumor cells, and the complex is internalized. Within the lysosomal compartment, the protein linker containing monomethyl auristatin E (MMAE) is enzymatically cleaved, releasing MMAE. MMAE inhibits microtubules, leading to cell cycle arrest and subsequent tumor cell death[1].
Glembatumumab vedotin exhibits cytotoxic activity against osteosarcoma cells at concentrations ranging from 1 to 125 μg/mL over a 96-hour period[2].

In human SK-MEL-2 and SK-MEL-5 melanoma xenograft models, Glembatumumab vedotin (CR011-vcMMAE) demonstrates both short-term antitumor effects (inhibiting tumor growth) and long-term effects (complete regression) when administered via intravenous injection at doses ranging from 1.25 to 80 mg/kg, every 4 days, for a duration of 16 days[3].