Drug intelligence / Profile preview

FE-DTBZ

Development stage
Preclinical
Lead developer
University of Pennsylvania
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

FE-DTBZ (9-fluoroethyl-9-desmethyl-dihydrotetrabenazine) is a fluorine-18 labeled small molecule radiopharmaceutical developed by researchers at the University of Pennsylvania and the University of Michigan. It functions as a high-affinity ligand for the vesicular monoamine transporter 2 (VMAT2), a protein responsible for the packaging of monoamine neurotransmitters into synaptic vesicles. As a positron emission tomography (PET) imaging agent, [18F]FE-DTBZ allows for the non-invasive quantification of VMAT2 density in the brain, which serves as a reliable biomarker for the integrity of dopaminergic neurons. It is primarily investigated for the diagnosis, differential diagnosis, and monitoring of neurodegenerative disorders characterized by monoaminergic loss, such as Parkinson's disease and Huntington's disease. The use of the fluorine-18 isotope provides a longer physical half-life (110 minutes) compared to carbon-11 labeled analogs, facilitating its distribution and use in routine clinical settings.

Other names
9-fluoroethyl-9-desmethyl-dihydrotetrabenazine(±)-FE-DTBZ9-fluoroethyl-9-desmethyl-DTBZFluorine-18 fluoroethyl-dihydrotetrabenazineFluorine18 fluoroethyl-dihydrotetrabenazineFluorine 18 fluoroethyl-dihydrotetrabenazine
02

Targets

VMAT2 (Vesicular monoamine transporter 2)

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