Drug intelligence / Profile preview

[18F]4

Development stage
Preclinical
Lead developer
Nemours Children’s Health
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

[18F]4 is a fluorine-18 labeled small-molecule radioligand targeting vascular endothelial growth factor receptor-3 (VEGFR-3). Designed as a fluorinated analog of the VEGFR-3 inhibitor SAR131675, it was developed by Nemours Children's Health for positron emission tomography (PET) imaging of tumor lymphatic activity and lymphangiogenesis. In vitro characterization shows that the (R)-enantiomer of the compound exhibits high binding affinity for VEGFR-3 and moderate-to-high selectivity over VEGFR-1 and VEGFR-2. Preliminary preclinical PET imaging in healthy mice demonstrates high uptake in the liver, intestine, and gallbladder, with low uptake in the brain.

Other names
(±)-[18F]4[18F]-4[18F]4[18F]SAR131675
02

Targets

VEGFR4 (Vascular endothelial growth factor Receptor-3)

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