Drug intelligence / Profile preview

[18F]PBR111

Development stage
Phase 1
Lead developer
Janssen Pharmaceutical
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[18F]PBR111 is a second-generation positron emission tomography (PET) radioligand that selectively binds to the 18 kDa translocator protein (TSPO), also known as the peripheral benzodiazepine receptor. TSPO is upregulated in activated microglia and astrocytes during neuroinflammatory processes. [18F]PBR111 enables in vivo visualization and quantification of neuroinflammation, making it a valuable tool for research into neurological diseases such as multiple sclerosis, Alzheimer's disease, schizophrenia, and other conditions involving microglial activation. The compound is labeled with fluorine-18 (half-life ~110 minutes), allowing for practical imaging protocols and distribution between sites without an on-site cyclotron. It has high signal specificity but its binding affinity can be affected by TSPO gene polymorphisms[1][3][8]. The agent is not FDA-approved but has been used in preclinical studies and clinical trials to assess neuroinflammation using PET imaging[6][9].

Other names
2-(6-chloro-2-(4-(3-fluoropropoxy)phenyl)imidazo(1,2-a)pyridin-3-yl)-N,N-diethylacetamide
02

Targets

TSPO (Translocator Protein (18 kDa))

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