Preferred Label : Anti-TF/Exatecan Antibody-drug Conjugate ADCE-T02;
NCIt synonyms : Anti-TF Antibody-drug Conjugate ADCE-T02; Topoisomerase-1 Inhibitor TF-ADC ADCE-T02; Anti-Tissue Factor ADC ADCE-T02; Anti-TF/Exatecan ADC ADCE-T02;
NCIt definition : An antibody-drug conjugate (ADC) comprised of Ab-754, a humanized immunoglobulin G1
(IgG1) monoclonal antibody against human tissue factor (TF; F3; coagulation factor
III; thromboplastin; CD142) conjugated, via the hydrophilic cleavable linker T1000,
to the camptothecin analog and cytotoxic DNA topoisomerase I inhibitor exatecan, with
potential antiangiogenic and antineoplastic activities. Upon administration of anti-TF/exatecan
ADC ADCE-T02, the monoclonal antibody moiety targets and binds to TF expressed on
tumor cells and ADCE-T02 is internalized. After internalization and cleavage, exatecan
targets and binds to DNA topoisomerase I, thereby stabilizing the cleavable complex
between topoisomerase I and DNA, resulting in DNA breaks, inhibition of DNA replication
and induction of apoptosis. This inhibits the proliferation of TF-expressing tumor
cells. In addition, ADCE-T02 induces a bystander effect, thereby further killing TF-negative
tumor cells. ADCE-T02 may also induce antibody-dependent cellular cytotoxicity (ADCC).
TF, a transmembrane protein and initiator of the coagulation cascade, is overexpressed
in many tumor cells and tumor-resident endothelial cells. Expression of TF is correlated
with metastasis, angiogenesis, tumor cell growth and tumor-associated thrombosis.
The hydrophilic moiety T1000 is used to overcome the hydrophobicity of conjugated
exatecan.;
Molecule name : ADCE T02; AMT 754; AMT-754; ADCE-T02;
Origin ID : C217658;
concept_is_in_subset
- has_target
