Preferred Label : Anti-ASCT2 Antibody-drug Conjugate MEDI7247;
NCIt synonyms : Anti-ASCT2/PBD ADC MEDI7247; Anti-ASCT2 ADC MEDI7247;
NCIt related terms : MEDI-7247;
NCIt definition : An antibody-drug conjugate (ADC) consisting of a human monoclonal antibody against
neutral amino acid transporter B(0) (ASCT2; SLC1A5) that is site-specifically conjugated,
via a protease-cleavable linker, to the cytotoxic, DNA minor-groove crosslinking agent
pyrrolobenzodiazepine (PBD) dimer, with potential antineoplastic activity. Upon administration
of anti-ASCT2 ADC MEDI7247, the antibody moiety targets and binds to ASCT2 expressed
on cancer cells. Upon antibody/antigen binding, internalization and linker cleavage,
the cytotoxic PBD moiety is released. In turn, the imine groups of the PBD moiety
bind to the N2 positions of guanines on opposite strands of DNA. This induces DNA
strand breaks, inhibits DNA replication, leads to G2/M cell cycle arrest, induces
cell death, and inhibits the proliferation of ASCT2-overexpressing tumor cells. ASCT2,
a neutral amino acid transporter that mediates the uptake of glutamine, is overexpressed
in a variety of cancer cell types.;
UNII : XZ66R08EI3;
Molecule name : MEDI 7247; MEDI7247;
NCI Metathesaurus CUI : CL524897;
Origin ID : C137821;
UMLS CUI : C4527229;
Semantic type(s)
- concept_is_in_subset
- has_target
