Preferred Label : Anti-B7-H3/Anti-EGFR Bispecific Antibody-drug Conjugate IBI3001;
NCIt synonyms : Anti-B7-H3/EGFR ADC IBI3001; Anti-B7-H3/Anti-EGFR Bispecific ADC IBI3001; Bispecific ADC IBI3001;
NCIt definition : An antibody-drug conjugate (ADC) composed of a bispecific antibody directed against
the tumor associated antigens (TAAs) B7-homologue 3 (B7-H3, CD276) and human epidermal
growth factor receptor (EGFR) that is site-specifically glycan-conjugated to the camptothecin
analog exatecan, with potential antineoplastic activity. Upon administration, anti-B7-H3/anti-EGFR
bispecific ADC IBI3001 targets and simultaneously binds to B7-H3 and EGFR expressed
on tumor cells. This blocks EGFR activation by ligands and EGFR-mediated signaling.
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 in B7-H3- and EGFR-expressing tumor cells.
In addition, IBI3001 causes a bystander effect, thereby killing both EGFR- and B7-H3-positive
cancer cells and EGFR- and B7-H3-negative cancer cells. EGFR, a receptor tyrosine
kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation
and tumor vascularization. B7-H3, a type I transmembrane protein and a member of the
B7 co-stimulatory protein superfamily, is overexpressed on certain tumor cell types
and on various immune cells. It is an immunoregulatory protein and negative regulator
of T-cell activation and its overexpression plays a key role in tumor cell invasion
and metastasis. B7-H3 and EGFR are co-expressed in multiple solid tumors.;
Molecule name : IBI 3001; IBI-3001;
Origin ID : C215075;
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