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drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
An antibody–drug conjugate targeting Trop-2 that delivers SN-38 (the active metabolite of irinotecan), a topoisomerase I inhibitor; internalization and linker cleavage release SN-38 to induce DNA damage and tumor cell death, with a potential bystander effect.
nci_thesaurus_concept_id
C102783
nci_thesaurus_preferred_term
Sacituzumab Govitecan
nci_thesaurus_definition
An antibody drug conjugate containing the humanized monoclonal antibody, hRS7, against tumor-associated calcium signal transducer 2 (TACSTD2 or TROP2) and linked to the active metabolite of irinotecan, 7-ethyl-10-hydroxycamptothecin (SN-38), with potential antineoplastic activity. The antibody moiety of sacituzumab govitecan selectively binds to TROP2. After internalization and proteolytic cleavage, SN-38 selectively stabilizes topoisomerase I-DNA covalent complexes, resulting in DNA breaks that inhibit DNA replication and trigger apoptosis. TROP2, also known as epithelial glycoprotein-1 (EGP-1), is a transmembrane calcium signal transducer that is overexpressed by a variety of human epithelial carcinomas; this antigen is involved in the regulation of cell-cell adhesion and its expression is associated with increased cancer growth, aggressiveness and metastasis.
drug_mesh_term
Sacituzumab Govitecan-hziy
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
Humanized anti-Trop-2 monoclonal antibody linked via a cleavable linker to SN-38 (active metabolite of irinotecan). After Trop-2 binding and internalization, linker cleavage releases SN-38, which inhibits topoisomerase I by stabilizing Topo I-DNA cleavage complexes, causing DNA damage, replication arrest, and apoptosis; extracellular release can produce a bystander killing effect.
drug_name
Sacituzumab govitecan
nct_id_drug_ref
NCT07018427