Glembatumumab is a fully humanIgG2monoclonal antibody directed against the extracellular structural domain ofGPNMBexpressed in human breastcancerand melanoma. Glembatumumab can be coupled to the microtubule inhibitor monomethylauristatinE to form glembatumumab vedotin. Glembatumumab vedotin is an antibody-drug coupling (ADC) with antitumor activity^[1].

Glembatumumab vedotin (CR011-vcMMAE) (0-2.5 μg/mL, 72 h) shows little growth inhibition in UACC62 melanoma cells without MEK inhibitor pretreatment at a concentration of 0.16 μg/mL, while the same dose of CR011-vcMMAE shows stronger growth inhibition in UACC62 cells pretreated with MEK inhibitor^[3].

Glembatumumab vedotin (i.v., 2.5 mg/kg, 3 times in 7 days) can inhibit tumor growth and is well tolerated in CB17SC scid^–/–female mice with sarcomas^[2].

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1020264-78-1

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