3BP-227

3BP-227 (also known as FPI-2059 or IPN01087) is a clinical-stage, DOTA-conjugated peptide radiopharmaceutical that acts as a selective antagonist of neurotensin receptor 1 (NTSR1). Originally developed by 3B Pharmaceuticals, the targeting ligand has been evaluated with various radionuclides for theranostic applications in oncology. Labeled with the beta-emitter lutetium-177 ([177Lu]Lu-IPN01087) or the alpha-emitter actinium-225 ([225Ac]Ac-FPI-2059), the compound delivers targeted cytotoxic radiation to NTSR1-expressing tumor cells, which are highly prevalent in ductal pancreatic adenocarcinoma, colorectal cancer, gastric cancer, Ewing sarcoma, and neuroendocrine differentiated prostate cancer. A diagnostic analogue labeled with indium-111 ([111In]In-FPI-2058) has also been developed for SPECT imaging to select patients with sufficient NTSR1 expression. Although AstraZeneca (which acquired Fusion Pharmaceuticals in 2024) terminated its development of FPI-2059 in December 2024 due to portfolio prioritization, 3B Pharmaceuticals continues to list the asset in its pipeline.

Other names

111In-FPI-2058111In-IPN-01087111In-IPN01087177Lu-3BP-227177Lu-IPN-01087177Lu-IPN01087225Ac-3BP-227225Ac-FPI-2059225Ac-IPN-01087actinium Ac 225 FPI-2059indium In 111 FPI-2058lutetium Lu 177-DOTA-IPN01087lutetium Lu 177-IPN01087