Drug intelligence / Profile preview

[111In]-FPI-2058

Development stage
Discontinued
Lead developer
AstraZeneca
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[111In]-FPI-2058 is a small molecule radiopharmaceutical imaging agent developed by 3B Pharmaceuticals GmbH, originally in collaboration with or acquired from Fusion Pharmaceuticals. It serves as the diagnostic imaging analogue to the therapeutic agent [225Ac]-FPI-2059. Both compounds target the neurotensin receptor 1 (NTSR1), a G protein-coupled receptor that is frequently overexpressed in various malignancies, including pancreatic ductal adenocarcinoma, colorectal cancer, gastric cancer, and head and neck squamous cell carcinoma, as well as Ewing sarcoma and neuroendocrine prostate cancer. [111In]-FPI-2058 utilizes the gamma-emitting isotope indium-111 to facilitate patient selection through SPECT imaging, ensuring that only patients with sufficient NTSR1 expression receive the corresponding alpha-particle therapy. A Phase 1 clinical trial (NCT05605522) evaluating this theranostic pair in advanced solid tumors was terminated.

Other names
Indium-111 FPI-2058Indium111 FPI-2058Indium 111 FPI-2058
02

Targets

NTR1 (Nitroreductase-1)

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