Drug intelligence / Profile preview

18F-fluoro-6-thia-heptadecanoic acid

Development stage
Unknown
Lead developer
Turku PET Centre
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Positron Emitters → Radiopharmaceuticals, Small Molecules
Administration
Intravenous, Oral
01

Overview

18F-fluoro-6-thia-heptadecanoic acid (18F-FTHA) is a radiolabeled long-chain fatty acid analog used as a positron emission tomography (PET) imaging tracer to evaluate fatty acid uptake and utilization (beta-oxidation) in vivo. Developed in 1991 by researchers at Forschungszentrum Jülich, 18F-FTHA enters cells via fatty acid transport proteins (FATPs) and CD36, where it is activated by long-chain acyl-CoA synthetase (ACSL) and transported into the mitochondria via carnitine palmitoyltransferase 1 (CPT1). Once inside the mitochondria, 18F-FTHA undergoes the initial steps of beta-oxidation but becomes metabolically trapped due to a sulfur atom at the 6th carbon position, which prevents further degradation. This metabolic trapping allows for the non-invasive quantification of fatty acid metabolism in tissues such as the myocardium, skeletal muscle, liver, and brown adipose tissue. It is currently being investigated in clinical trials for imaging lymphatic obstruction and assessing metabolic alterations in obesity and type 2 diabetes.

Other names
14-(R,S)-[18F]fluoro-6-thia-heptadecanoic acid14-fluoro-6-thiaheptadecanoic acid14-fluorine-18-fluoro-6-thia-heptadecanoic acid14(R,S)-[18F]-fluoro-6-thiaheptadecanoic acid14(R,S)-[18F]fluoro-6-thia-heptadecanoic acid18F-6-thia-14-fluoro-heptadecanoic acid18F-FTHAFTHA
02

Targets

SLC7A1 (Cationic amino acid transporter 1)ACS (Acetyl-CoA synthetase)CD36 (CD36 antigen)

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