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177Lu-FAPI-TRX
- Development stage
- Preclinical
- Lead developer
- University of California, San Francisco
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Small Molecules
- Administration
- Intravenous
01
Overview
177Lu-FAPI-TRX is a preclinical-stage radioligand therapy (RLT) developed by the University of California, San Francisco (UCSF). It targets fibroblast activation protein (FAP), which is highly expressed in the tumor microenvironment of various aggressive cancers. The drug incorporates a conditionally activated 1,2,4-trioxolane (TRX)-based linker that reacts with free iron in its reduced, ferrous (Fe2+) state to produce carbon-centered radicals that rapidly crosslink endosomal or cytosolic biomolecules. This covalent anchoring mechanism prolongs the retention of the therapeutic Lutetium-177 (177Lu) isotope within the tumor, delivering higher radiation accumulation and superior antitumor efficacy compared to non-TRX-engineered radioligands like 177Lu-FAPI-46.
- Other names
- 177Lu-labeled FAPI-TRXLu-177-FAPI-TRXLu177-FAPI-TRXLu 177-FAPI-TRX
02
Targets
FAP (Fibroblast activation protein alpha)
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