Preferred Label : Anti-TROP2 Antibody-drug Conjugate ESG401;
NCIt synonyms : Anti-TROP2/SN-38 ADC ESG401; Anti-TROP-2 ADC ESG401; Anti-TROP2 ADC ESG401; ADC ESG401; Anti-TROP2/SN-38 Antibody-drug Conjugate ESG401;
NCIt definition : An antibody-drug conjugate (ADC) composed of sacituzumab, a humanized immunoglobulin
G1 (IgG1) monoclonal antibody targeting the tumor-associated antigen (TAA) trophoblast
cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2;
TROP-2; TACSTD2; GA733-1; M1S1) covalently linked via the protease-labile linker maleimidocaproyl-valine-citrulline-p-aminobenzyloxycarbonyl
(MC-VC-PABC), to the topoisomerase-1 inhibitor and the active metabolite of irinotecan
7-ethyl-10-hydroxycamptothecin (SN-38), with potential antineoplastic activity. Upon
administration of the anti-TROP-2 ADC ESG401, the anti-TROP-2 antibody targets and
binds to TROP-2 expressed on tumor cells. Upon binding, internalization and proteolytic
cleavage, SN-38 is released, selectively stabilizes topoisomerase I-DNA covalent complexes,
resulting in DNA breaks and an inhibition of DNA replication and induction of apoptosis.
This inhibits the proliferation of TROP-2-expressing tumor cells. TROP-2 is a transmembrane
protein overexpressed in various tumors. Its expression is associated with enhanced
tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.;
Molecule name : ESG-401; ESG 401;
Origin ID : C216087;
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