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drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate
drug_description
An antibody-drug conjugate targeting Trop-2; a humanized anti–Trop-2 IgG linked to SN-38 (active metabolite of irinotecan), a topoisomerase I inhibitor that is released upon internalization to induce DNA damage and apoptosis.
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
Humanized anti–TROP2 IgG linked to SN-38. Binds TROP2 on tumor cells, is internalized, and releases SN-38 after linker cleavage. SN-38 inhibits topoisomerase I by stabilizing Topo I–DNA complexes, causing DNA strand breaks, impaired replication, and apoptosis; may exert a bystander effect due to membrane-permeable payload.
drug_name
Sacituzumab govitecan
nct_id_drug_ref
NCT06528483