drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate (ADC)
drug_description
TROP-2–directed antibody–drug conjugate delivering SN-38 (topoisomerase I inhibitor).
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-TROP2 monoclonal antibody linked to SN-38 (active metabolite of irinotecan). After binding TROP2 on tumor cells and internalization, the linker is cleaved to release SN-38, which inhibits topoisomerase I by stabilizing the Topo I–DNA complex, leading to DNA damage, replication arrest, and apoptosis (with potential bystander effect).
drug_name
Sacituzumab govitecan
nct_id_drug_ref
NCT06145308