Drug intelligence / Profile preview

floretyrosine (18F)

Development stage
Approved
Lead developer
Curium
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous
01

Overview

floretyrosine (18F) (also known as 18F-FET or O-(2-[18F]fluoroethyl)-L-tyrosine) is a radioactive diagnostic radiopharmaceutical used with positron emission tomography (PET) imaging. It is a synthetic amino acid analogue labeled with the positron-emitting radioisotope fluorine-18. Floretyrosine (18F) is actively transported into cells via L-type amino acid transporters (specifically LAT1 and LAT2), which are significantly upregulated in tumor cells, particularly gliomas, compared to healthy brain tissue. Unlike 18F-FDG, floretyrosine (18F) has low uptake in normal brain tissue and inflammatory cells, providing a high tumor-to-background ratio. It is primarily indicated to differentiate recurrent or progressive glioma from treatment-related changes (such as pseudoprogression or radiation necrosis) in adult and pediatric patients. It is also being evaluated for the diagnosis of brain metastases.

Brand names
IASOglioPixclara
Other names
18F-FET2-fluoroethyltyrosine F-18FET F-18floretyrosine (18F)floretyrosine F 18floretyrosine F-18floretyrosine F18fluoroethyl-L-tyrosine (18F)fluoroethyltyrosine F-18L-tyrosine, O-[2-(fluoro-18F)ethyl]-O-(2-[18F]fluoroethyl)-L-tyrosineO-(2-[¹⁸F]fluoroethyl)-L-tyrosineO-[2-(fluoro-18F)ethyl]-L-tyrosine
02

Targets

SLC7A5 (Large neutral amino acid transporter small subunit 1)LAT2 (Linker for activation of T cells family member 2)

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