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[177Lu]Lu-RTX-2358
- Development stage
- Phase 1
- Lead developer
- Ratio Therapeutics
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Beta-minus Emitters → Radiopharmaceuticals, Gamma Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
[177Lu]Lu-RTX-2358 is a therapeutic radiopharmaceutical consisting of the beta-emitting radioisotope Lutetium-177 conjugated to a ligand (RTX-2358) that targets Fibroblast Activation Protein (FAP). FAP is a cell-surface serine protease that is highly expressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment of various solid tumors, including non-small cell lung cancer (NSCLC), while showing minimal expression in healthy adult tissues. By binding specifically to FAP, the drug delivers targeted ionizing radiation to the tumor site, causing DNA damage and cell death in both the stromal and adjacent malignant cells. It is currently being evaluated in clinical trials, often in combination with immune checkpoint inhibitors (PD-1 inhibitors), to investigate potential synergistic effects between targeted radiotherapy and immunotherapy in patients with FAP-positive metastatic cancers.
- Other names
- 177Lu-RTX-2358Lutetium-177 RTX-2358Lutetium177 RTX-2358Lutetium 177 RTX-2358
02
Targets
FAP (Fibroblast activation protein alpha)
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