Drug intelligence / Profile preview

DPA-714

Development stage
Phase 2
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

DPA-714 is a small molecule ligand that selectively binds to the 18 kDa translocator protein (TSPO), formerly known as the peripheral benzodiazepine receptor. TSPO is upregulated in activated microglia and other cell types at sites of neuroinflammation and central nervous system pathology. DPA-714, particularly in its fluorine-labeled form ([18F]DPA-714), is used as a radiotracer for positron emission tomography (PET) imaging to non-invasively assess neuroinflammation in various neurological diseases, including Parkinson’s disease, Alzheimer’s disease, autoimmune encephalitis, multiple sclerosis, fibromyalgia, and chronic fatigue syndrome. The compound displays high affinity for TSPO (dissociation constant ~7 nM) and can stimulate pregnenolone synthesis. It has been evaluated preclinically and clinically for its ability to detect active disease processes by visualizing TSPO expression in the brain and peripheral organs[1][5][6][7][8].

Other names
N,N-diethyl-2-(2-(4-(2-[18F]-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide
02

Targets

TSPO (Translocator Protein (18 kDa))

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