drug_type
RELEVANT_DRUG
intervention_type
Drug
drug_description
An anti-TROP2 antibody-drug conjugate composed of a TROP2-targeting monoclonal antibody linked via a cleavable peptide to the topoisomerase I inhibitor exatecan; binds TROP2 on tumor cells, is internalized, and releases exatecan to induce DNA damage, S-phase arrest, and apoptosis.
nci_thesaurus_concept_id
C207806
nci_thesaurus_preferred_term
Anti-TROP2 Antibody-drug Conjugate OBI-992
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1), conjugated to a topoisomerase-1 inhibitor (TOP1i; TOP-Ii) via a hydrophilic, enzyme-cleavable linker, with potential antineoplastic activity. Upon administration of anti-TROP2 ADC OBI-992, the anti-TROP2 antibody moiety targets and binds to TROP2 expressed on tumor cells. Upon binding, internalization and linker cleavage, the TOP1i moiety is released, binds to TOP1 and inhibits DNA topoisomerase I activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of TROP2-expressing tumor cells. TROP2 is a transmembrane protein overexpressed in various tumors. Its expression is associated with enhanced tumor aggressiveness, metastasis, drug resistance and increased tumor cell survival.
drug_mesh_term
Antibody-Drug Conjugates
drug_category
ANTIBODY DRUG CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
TROP2-targeting antibody-drug conjugate that binds TROP2 on tumor cells, is internalized, and releases the topoisomerase I inhibitor exatecan via a cleavable linker; the released payload inhibits TOP1, causing DNA damage, S-phase arrest, and apoptosis in TROP2-expressing tumor cells.
drug_name
OBI-992
nct_id_drug_ref
NCT06480240