Drug intelligence / Profile preview

[18F]RP-115

Development stage
Phase 2
Lead developer
University of California, San Francisco
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[18F]RP-115 is a fluorine-18 labeled radiopharmaceutical compound developed as a positron emission tomography (PET) imaging tracer. It is a methyl ester prodrug that undergoes metabolic saponification in the central nervous system to generate its carboxylic acid form, which selectively binds to the excitatory amino acid transporter 2 (EAAT2) protein. EAAT2 is abundantly expressed by astrocytes in the brain and plays a key role in glutamate regulation. The primary clinical application of [18F]RP-115 is as an investigational PET imaging agent for mapping EAAT2 expression and function, with particular focus on neuroinflammation and early detection of Alzheimer’s disease. First-in-human studies have demonstrated that intravenous administration of [18F]RP-115 is safe and well-tolerated, with favorable biodistribution and organ dosimetry profiles[1][3][4][9].

Other names
methyl N-(4-([18F]7-fluoro-9H-fluoren-2-yl)asparaginate
02

Targets

SLC1A2 (Glutamate Transporter 1)

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