Drug intelligence / Profile preview

[18F]fluoro-PEG-folate

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

Overview

**[18F]fluoro-PEG-folate** is a radiopharmaceutical PET tracer designed for **targeted imaging of folate receptor (FR)-expressing cells**, primarily for the detection of inflammation and cancer. It binds both FR-α (commonly overexpressed in certain cancers) and FR-β (on activated macrophages in inflamed tissues). The radiotracer is synthesized by conjugating a fluorine-18 label (via a polyethylene glycol [PEG] linker) to folic acid, enhancing its pharmacokinetics and specificity. In clinical studies, [18F]fluoro-PEG-folate demonstrated rapid blood clearance, low background uptake, and high target-to-background ratios, making it particularly effective for imaging inflamed joints in rheumatoid arthritis and potentially other inflammatory and oncologic conditions. Its mechanism of action is **receptor-mediated targeting** of FR-expressing cells, facilitating sensitive whole-body PET imaging for diagnostic and monitoring purposes[2][1][3].

Other names
[18F]fluoro-PEG-folate
02

Targets

FOLR1 (FRα)FOLR2 (Folate receptor beta)

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