Drug intelligence / Profile preview

(S)-[18F]FBFP

Development stage
Phase 1
Lead developer
Washington University in St. Louis
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

(S)-[18F]FBFP is a fluorine-18 labeled radiopharmaceutical that serves as a positron emission tomography (PET) tracer for the sigma-1 receptor (σ1R). The sigma-1 receptor is a molecular chaperone located in the endoplasmic reticulum that modulates various cellular processes, including calcium signaling and protein folding. It is highly expressed in the central nervous system and is implicated in the pathophysiology of neurodegenerative diseases, such as Alzheimer's and Parkinson's, as well as psychiatric disorders like major depression. (S)-[18F]FBFP is the S-enantiomer of a piperazine derivative, chosen for its high affinity and selectivity for σ1R over the sigma-2 receptor. In clinical research, it is used to non-invasively map and quantify σ1R density in the human brain, providing insights into disease mechanisms and facilitating the development of σ1R-targeted therapies by measuring receptor occupancy.

Other names
(S)-1-(3-bromo-4-[18F]fluorobenzyl)-4-[(2-fluorophenyl)methyl]piperazine[18F]FBFP
02

Targets

SIGMAR1 (Sigma non-opioid intracellular receptor 1)

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