Background：Belantamab mafodotin also known as GSK2857916 is a humanized, IgG1 antibody-drug conjugate ADC that binds specifically to BCMA. The parent anti-BCMA antibody GSK2857914 is produced in an afucosylated form and is conjugated to the microtubule polymerization inhibitor MMAF, via a protease-resistant maleimidocaproyl mc linker, to produce the GSK2857916 ADC molecule. Upon binding to the cell surface, GSK2857916 is rapidly internalized and active cytotoxic drug cys-mcMMAF is released inside the cell causing cell-cycle arrest and apoptosis. Furthermore, the afucosylation of GSK2857916 leads to enhanced binding to FcγRIIIa receptors on the surface of immune effector cells, recruitment of immune cells, and antibody-dependent cellular cytotoxicity and phagocytosis ADCC and ADCP, respectively. This dual mechanism of action enables improved efficacy by targeting both dividing via ADC and non-dividing via ADCC/ADCP tumor cells. Recently, belantamab mafodotin was approved under the name BLENREP in the United States and European Union for the treatment of patients with relapsed or refractory multiple myeloma.
Alternative Names：2857916, GSK2857916, J6M0, J6M0-mcMMAF,
