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[177Lu]Lu-TEFAPI-06
- Development stage
- Phase 1
- Lead developer
- Lanzhou University
- Modality
- Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
[177Lu]Lu-TEFAPI-06 is a novel radiopharmaceutical developed by Lanzhou University Second Hospital for the treatment of advanced metastatic solid tumors. It is a radioligand therapy consisting of TEFAPI-06, a fibroblast activation protein inhibitor (FAPI) derived from FAPI-04, which is conjugated to a 4-(p-iodophenyl) butyric acid moiety serving as an albumin binder. This modification is designed to prolong blood circulation and enhance tumor accumulation and retention compared to earlier FAPI tracers. The drug targets fibroblast activation protein (FAP), which is highly expressed in the tumor microenvironment of various solid tumors. By delivering the beta-emitting radioisotope lutetium-177 directly to FAP-expressing cells, it provides targeted radiotherapy. Preclinical studies have demonstrated significant tumor growth inhibition in pancreatic cancer models, and it is currently being evaluated in a first-in-human trial for safety, dosimetry, and preliminary efficacy.
- Other names
- [177Lu]-TEFAPI-06Lutetium (177Lu) TEFAPI-06
02
Targets
FAP (Fibroblast activation protein alpha)
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