Drug intelligence / Profile preview

fluorine-18 fluoropropyl-(±)-dihydrotetrabenazine

Development stage
Unknown
Lead developer
Avid Radiopharmaceuticals
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Fluorine-18 fluoropropyl-(±)-dihydrotetrabenazine, also known as [18F]6b, is a racemic small molecule radiopharmaceutical developed as a positron emission tomography (PET) imaging agent. It was developed by the University of Pennsylvania in collaboration with Avid Radiopharmaceuticals (now a subsidiary of Eli Lilly). The tracer is a fluoropropyl analog of dihydrotetrabenazine (DTBZ) and specifically targets the vesicular monoamine transporter 2 (VMAT2), which is responsible for transporting monoamine neurotransmitters into synaptic vesicles. The density of VMAT2 serves as a biomarker for the integrity of monoaminergic neurons, which degenerate in neurodegenerative diseases such as Parkinson's disease and Huntington's disease. While the racemic mixture demonstrated high binding affinity and favorable pharmacokinetics in preclinical studies, subsequent clinical development primarily focused on the optically pure active enantiomer, [18F]FP-(+)-DTBZ, also known as AV-133 or Florbenazine.

Other names
fluorine-18 fluoropropyl-dihydrotetrabenazinefluorine18 fluoropropyl-dihydrotetrabenazinefluorine 18 fluoropropyl-dihydrotetrabenazineracemic 18F-FP-DTBZracemic18F-FP-DTBZracemic-18F-FP-DTBZ18F-fluoropropyl-DTBZ
02

Targets

VMAT2 (Vesicular monoamine transporter 2)

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