drug_type
RELEVANT_DRUG
intervention_type
Antibody-drug conjugate (Drug)
drug_description
An antibody-drug conjugate composed of a humanized anti–Trop-2 IgG1 monoclonal antibody linked via a cleavable linker to SN-38 (the active metabolite of irinotecan). After binding Trop-2 on tumor cells and internalization, it releases SN-38 to inhibit topoisomerase I, inducing DNA damage and apoptosis; the cleavable linker enables bystander killing, with potential Fc-mediated effector functions.
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 IgG1 antibody delivers the topoisomerase I–inhibiting payload SN-38 via a cleavable linker; after Trop-2 binding and internalization, SN-38 is released to stabilize Topo I–DNA complexes, causing DNA damage and apoptosis, with a cleavable linker enabling bystander killing and potential Fc-mediated effector functions.
drug_name
Sacituzumab govitecan-hziy
nct_id_drug_ref
NCT06477419