Anti-TF/Exatecan Antibody-drug Conjugate ADCE-T02

**Semantic type:** Pharmacologic Substance

**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.

**Synonyms:** - ADCE T02 - ADCE-T02 - ADCET02 - AMT 754 - AMT-754 - AMT754 - Anti-TF Antibody-drug Conjugate ADCE-T02 - Anti-TF/Exatecan ADC ADCE-T02 - Anti-Tissue Factor ADC ADCE-T02 - Topoisomerase-1 Inhibitor TF-ADC ADCE-T02