Preferred Label : Anti-GCC Antibody-Drug Conjugate TAK-164;
NCIt synonyms : TAK 164; Anti-GCC ADC TAK-164;
NCIt related terms : TAK-164;
NCIt definition : An antibody-drug conjugate (ADC) comprised of a full-length, fully-human immunoglobulin
G1 (IgG1) monoclonal antibody (mAb) directed against the extracellular domain of guanylyl
cyclase C (GCC; GUCY2C), conjugated using the peptide-linked indolino-benzodiazepine
DNA alkylator DGN549 (IGN-P1), with potential antineoplastic activity. Upon intravenous
administration of TAK-164, the antibody moiety selectively binds to GCC-expressing
cells. Upon antibody/antigen binding and internalization, the cytotoxic DGN549 payload
is released and binds to guanine residues on opposing 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 GCC-expressing cells. GCC, a transmembrane
receptor normally found on intestinal cells and dopamine neurons in the brain, is
overexpressed on the surface of certain tumor cells.;
UNII : QCA97P3GSS;
Molecule name : TAK-164;
NCI Metathesaurus CUI : CL935871;
Origin ID : C156707;
UMLS CUI : C4745004;
Semantic type(s)
- concept_is_in_subset
- has_target
