drug_type
RELEVANT_DRUG
intervention_type
Antibody–drug conjugate (ADC)
drug_description
An intravenous antibody–drug conjugate targeting Trop-2 (TACSTD2); the monoclonal antibody binds Trop-2 on tumor cells, is internalized, and releases a cytotoxic payload intracellularly to induce cancer cell death. Dosed every 21 days; being evaluated in a first-in-human Phase I study for MTD/DLT, PK, safety, and preliminary antitumor activity in advanced solid tumors.
nci_thesaurus_concept_id
C204169
nci_thesaurus_definition
An antibody-drug conjugate (ADC) composed of a humanized immunoglobulin G1 (IgG1) monoclonal antibody targeting the tumor-associated antigen (TAA) trophoblast cell surface protein 2 (trophoblast antigen 2; calcium signal transducer 2; TROP2; TROP-2; TACSTD2; GA733-1; M1S1) linked, via a cleavable linker, to a topoisomerase-1 inhibitor, with potential antineoplastic activity. Upon administration of anti-TROP-2 ADC HS-20105, the anti-TROP-2 antibody targets and binds to TROP-2 expressed on tumor cells. Upon binding, internalization and linker cleavage, the topoisomerase-1 inhibitor is released, and inhibits DNA topoisomerase-1 activity, thereby inhibiting DNA replication and resulting in cell cycle arrest and tumor cell apoptosis. This inhibits the proliferation of TROP-2-expressing tumor cells. TROP-2 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
Humanized IgG1 anti–TROP-2 antibody–drug conjugate that binds TROP-2 on tumor cells, is internalized, and via a cleavable linker releases a topoisomerase I inhibitor payload intracellularly, inhibiting DNA replication and inducing cell cycle arrest and apoptosis in TROP-2–expressing cancers.
drug_name
HS-20105
nct_id_drug_ref
NCT06144723