Glembatumumab

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-drug coupling (ADC) with antitumor activity[1].

Research Areas >> Cancer

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].

[1]. 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.

[2]. 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.

[3]. 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.