drug_type
RELEVANT_DRUG
intervention_type
Radionuclide therapy
drug_description
A fibroblast activation protein (FAP)-targeted radiopharmaceutical in which the FAP-binding ligand LNC1004 is labeled with the beta-emitting radionuclide lutetium-177; it binds FAP on cancer-associated fibroblasts and delivers localized beta radiation, causing DNA damage with cross-fire effects on nearby tumor cells.
nci_thesaurus_concept_id
C200128
nci_thesaurus_definition
A radioconjugate consisting of an Evans blue (EB) modified fibroblast activation protein inhibitor (FAPi), conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecane tetraacetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177, with potential antineoplastic activity. Upon administration of lutetium Lu 177 LNC1004, the FAPi moiety targets and binds to FAP-expressing cancer-associated fibroblasts (CAFs). Upon binding and internalization, the radioconjugate specifically delivers a cytotoxic dose of beta radiation to FAP-expressing CAFs. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME).
drug_mesh_term
Radiopharmaceuticals
drug_category
RADIOPEPTIDE CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
EB-modified FAP inhibitor LNC1004 is chelated with DOTA and labeled with lutetium-177; after binding to fibroblast activation protein on cancer-associated fibroblasts, the complex is internalized and delivers beta radiation that induces DNA damage and cell death in FAP-expressing stromal cells with cross-fire effects killing adjacent tumor cells.
drug_name
177Lu-LNC1004
nct_id_drug_ref
NCT05723640