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drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate
drug_description
A Trop-2-targeted antibody-drug conjugate that delivers SN-38 (irinotecan's active metabolite), a topoisomerase I inhibitor, causing 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
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
A Trop-2-targeted antibody-drug conjugate that binds Trop-2 on tumor cells, is internalized, and releases SN-38 (irinotecan's active metabolite). SN-38 inhibits topoisomerase I by stabilizing Topo I-DNA complexes, leading to DNA breaks, inhibition of replication, and apoptosis, with a potential bystander killing effect.
drug_name
Sacituzumab govitecan
nct_id_drug_ref
NCT06682728