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Glembatumumab vedotin
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Glembatumumab vedotin : ウィキペディア英語版
Glembatumumab vedotin

Glembatumumab vedotin (also known as CDX-011 and CR011-vcMMAE) is an antibody-drug conjugate (ADC) that targets cancer cells expressing transmembrane glycoprotein NMB (GPNMB).
In May 2010, the U.S FDA granted Fast Track designation to CDX-011 for the treatment of advanced, refractory or resistant GPNMB-expressing breast cancer.
==Structure and mechanism==
The fully human IgG2 monoclonal antibody glembatumumab (CR011) is linked to monomethyl auristatin E (MMAE).
It uses a valine-citrulline enzyme-cleavable linker.〔(【引用サイトリンク】title=The EMERGE study )
The linkage is stable in the bloodstream. The antibody binds to GPNMB on the cancer cells, the ADC is internalised, the linkage is broken and MMAE is released to kill the cell.〔
In preclinical studies glembatumumab vedotin was capable of killing GPNMB expressing melanoma and breast cancer cells ''in vitro'' and inducing partial or complete regression of GPNMB-expressing tumors in mouse models.〔

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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