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XTR022 is an innovative theranostic radiopharmaceutical candidate developed by Sinotau Pharmaceutical Group, targeting **Fibroblast Activation Protein (FAP)**. The drug utilizes a Fibroblast Activation Protein Inhibitor (FAPI) ligand modified with an **Evans Blue (EB)** moiety. This EB modification allows the molecule to bind reversibly to serum albumin, significantly extending its blood circulation half-life and increasing accumulation within the tumor microenvironment compared to first-generation FAPI tracers. When labeled with the beta-emitting radioisotope **Lutetium-177 (177Lu)**, XTR022 serves as a targeted radionuclide therapy for various advanced solid tumors where FAP is highly expressed in the cancer-associated fibroblasts of the stroma. It is currently being evaluated in investigator-initiated trials (IITs) and early-stage clinical studies in China, positioning it as a potential first-in-class or best-in-class FAP-targeted therapy in the region.
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