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IPN-1087 is a small molecule radiopharmaceutical that targets neurotensin receptor 1 (NTSR1), a protein overexpressed in multiple solid tumor types including pancreatic ductal adenocarcinoma, colorectal cancer, gastric cancer, head and neck squamous cell carcinoma, neuroendocrine prostate cancer, and Ewing sarcoma. It was originally developed as a lutetium-177-based beta-emitting radiopharmaceutical for targeted therapy of these tumors. The drug binds to NTSR1 on tumor cells delivering localized radiation to induce tumor cell death. Fusion Pharmaceuticals acquired IPN-1087 from Ipsen in April 2021 and has converted it into an alpha-emitting radioconjugate called FPI-2059 by labeling with actinium-225 for enhanced therapeutic efficacy at much lower doses. Clinical studies of IPN-1087 showed promising early safety data and good tumor uptake across multiple solid tumors[1][2][3][5][6][8].
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