drug_type
RELEVANT_DRUG
intervention_type
Radiopharmaceutical
drug_description
A FAP-targeted radiopharmaceutical: a 177Lu-labeled small-molecule FAPI ligand that selectively binds fibroblast activation protein on cancer-associated fibroblasts in the tumor stroma and delivers beta-emitting lutetium-177 to induce localized DNA double-strand breaks and cell death, with crossfire irradiation of adjacent tumor cells.
nci_thesaurus_concept_id
C206262
nci_thesaurus_definition
A radioconjugate composed of XT117, a fibroblast activation protein inhibitor (FAPi), conjugated to the beta-emitting radioisotope lutetium Lu 177 (177Lu), with potential antineoplastic activity against FAP-expressing cancer-associated fibroblasts (CAFs). Upon administration, lutetium Lu 177 XT117 targets and binds to FAP-expressing CAFs. Upon binding, FAP-expressing CAFs are destroyed by 177Lu through the specific delivery of beta particle radiation. FAP, a cell surface protein, is overexpressed on CAFs in the tumor microenvironment (TME) of various cancers.
drug_mesh_term
Radiopharmaceuticals
drug_category
RADIOPEPTIDE CONJUGATE
drug_class
Conjugate
drug_delivery_route
Intravenous
drug_mechanism_of_action
A 177Lu-labeled FAP inhibitor ligand that binds fibroblast activation protein on cancer-associated fibroblasts and delivers beta-emitting lutetium-177 to induce DNA double-strand breaks and cell death, with crossfire irradiation of adjacent tumor cells in the tumor microenvironment.
drug_name
[177Lu]Lu-XT117
nct_id_drug_ref
NCT06197139