Drug intelligence / Profile preview

(2S,4R)-4-fluoroglutamine

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

Overview

(2S,4R)-4-fluoroglutamine (commonly utilized as the fluorine-18 radiolabeled PET tracer [18F]-(2S,4R)-4-fluoroglutamine or 18F-FGln) is an investigational diagnostic radiopharmaceutical and L-glutamine analog developed for positron emission tomography (PET) imaging of tumor glutamine flux and metabolism. Many aggressive cancers exhibit 'glutamine addiction,' upregulating glutamine transporters and glutaminolysis to support rapid proliferation. (2S,4R)-4-fluoroglutamine is actively transported into tumor cells primarily via the sodium-dependent neutral amino acid transporter ASCT2 (encoded by SLC1A5) and system L transporters. Once inside the cell, it serves as a metabolic probe to measure intracellular glutamine pool size and glutaminolysis rates, providing a noninvasive method to characterize tumor metabolic heterogeneity, stage malignancies (such as lung cancer, breast cancer, and gliomas), and monitor response to glutamine-targeting therapies (e.g., glutaminase inhibitors).

Other names
(18F) 4-L-fluoroglutamine (2S,4R)(18F)4-L-fluoroglutamine(18F)FGN(2S,4R)-2,5-diamino-4-(fluoro-18F)-5-oxopentanoic acid(2S,4R)-4-fluoroglutamine F-18(2S,4R)-4FGIN(4R)-4-(18F)fluoro-L-glutamine18F-(2S,4R)4-fluoroglutamine18F-FGLN18F-fluoroglutamine4-FGln4-fluoroglutamineFGlnL-glutamine, 4-(fluoro-18F)-, (4R)-[18F]-(2S,4R)-4-fluoroglutamine[18F]4-FGlnfluoroglutamine F-18
02

Targets

GLS1 (Glutaminase 1)SLC7A5 (Large neutral amino acid transporter small subunit 1)SLC6A19 (Na+-dependent system B0 transporter)

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