Drug intelligence / Profile preview

[177Lu]Lu-DOTA-4P(FAPI)4

Development stage
Preclinical
Lead developer
Xiamen University
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

[177Lu]Lu-DOTA-4P(FAPI)4 is a preclinical-stage radiolabeled fibroblast activation protein (FAP) inhibitor (FAPI) tetramer designed for targeted radioligand therapy of FAP-expressing tumors. Developed by researchers at Xiamen University, the agent utilizes a polyvalent tetrameric structure based on FAPI-46 conjugated to a DOTA chelator and radiolabeled with the beta-emitting radionuclide lutetium-177 (177Lu). By exploiting the polyvalency effect, the tetramer exhibits significantly higher tumor uptake, longer tumor retention, and slower clearance compared to its monomeric and dimeric counterparts. In preclinical models of FAP-positive tumors (such as HT-1080-FAP and U87MG xenografts), [177Lu]Lu-DOTA-4P(FAPI)4 demonstrated robust antitumor efficacy and tumor growth suppression.

Other names
177Lu-DOTA-4P(FAPI)4177Lu-labeled FAPI tetramerlutetium Lu 177 DOTA-4P(FAPI)4lutetium-177 DOTA-4P(FAPI)4
02

Targets

FAP (Fibroblast activation protein alpha)

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