Glembatumumab vedotin (CDX-011) is an antibody-activated small molecule coupling, Glembatumumab vedotin has potent anticancer effects and can be used in the study of triple negative breast cancer (TNBC).

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].