Glembatumumab is a fully human IgG2 monoclonal antibody directed against the extracellular structural domain of GPNMB expressed in human breast cancer and melanoma. Glembatumumab can be coupled to the microtubule inhibitor monomethyl auristatin E to form glembatumumab vedotin. Glembatumumab vedotin is an antibody-agent coupling (ADC) with antitumor activity.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Naumovski L, et al. Glembatumumab vedotin, a conjugate of an anti-glycoprotein non-metastatic melanoma protein B mAb and monomethyl auristatin E for the treatment of melanoma and breast cancer. Curr Opin Mol Ther. 2010 Apr;12(2):248-57.  [Content Brief]

  . E Anders Kolb, et al. Initial testing (stage 1) of glembatumumab vedotin (CDX-011) by the pediatric preclinical testing program. Pediatr Blood Cancer. 2014 Oct;61(10):1816-21.  [Content Brief]

  . Xiaozhong Qian, et al. Pharmacologically enhanced expression of GPNMB increases the sensitivity of melanoma cells to the CR011-vcMMAE antibody-drug conjugate. Mol Oncol. 2008 Jun;2(1):81-93.  [Content Brief]