Drug intelligence / Profile preview

[18F]GPR39

Development stage
Preclinical
Lead developer
Wake Forest University School of Medicine
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

[18F]GPR39 is a fluorine-18-labeled positron emission tomography (PET) radiotracer designed for the non-invasive, real-time imaging of G protein-coupled receptor 39 (GPR39) expression levels in the brain. Developed by researchers at the Wake Forest University School of Medicine, the tracer is aimed at investigating zinc dyshomeostasis, a hallmark of Alzheimer's disease and related dementias that drives neurodegenerative pathways such as tau hyperphosphorylation, neuroinflammation, and oxidative stress. GPR39 is a zinc-sensing receptor that plays a key role in maintaining zinc homeostasis, and its dysregulation is linked to the accumulation of amyloid-beta and tau pathology. [18F]GPR39 demonstrates high affinity and specificity for GPR39, reliable blood-brain barrier penetration, and stability in human serum, making it a promising tool for monitoring GPR39 expression and target engagement during therapeutic interventions.

Other names
18F-GPR3918F-GPR39-2.1
02

Targets

GPR39 (G protein-coupled receptor 39)

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