Preferred Label : Anti-ADAM9/Exatecan Antibody-drug Conjugate MGC028;
NCIt synonyms : Anti-ADAM9 ADC MGC028;
NCIt definition : An antibody-drug conjugate (ADC) composed of a humanized monoclonal antibody directed
against the tumor-associated antigen (TAA) a disintegrin and metalloproteinase domain
9 (ADAM9), site-specifically conjugated at asparagine 297 of the heavy chain through
enzymatic glycan remodeling, via a cleavable bicyclononyne carbamoyl sulfamide Val-Ala-PABC
linker, to the cytotoxic DNA topoisomerase I inhibitor exatecan, with potential antineoplastic
activity. Upon administration of anti-ADAM9 ADC MGC028, the anti-ADAM9 monoclonal
antibody moiety targets and binds to ADAM9 on tumor cells. Upon binding, internalization,
and linker cleavage, exatecan is released and inhibits DNA topoisomerase I activity,
thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell
apoptosis. MGC028 is also able to induce a bystander effect on neighboring cells in
the tumor environment. This further inhibits the proliferation of tumor cells. ADAM9,
belonging to the ADAM family of proteases, plays a key role in cytokine and growth
factor shedding and cell migration. It is overexpressed on multiple solid tumors while
minimally expressed on normal tissue. Dysregulation of ADAM9 has been implicated in
tumor progression, migration and metastasis. Its expression is correlated with poor
prognosis. MGC028 does not bind Fc-gamma receptors.;
Molecule name : MGC 028; MGC-028;
Origin ID : C217125;
concept_is_in_subset
- has_target
