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Fluorodeoxyglucose (18F)

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Fluorodeoxyglucose (18F)

[18
F
]Fluorodeoxyglucose
(INN), or fluorodeoxyglucose F 18 (USAN and USP), also commonly called fluorodeoxyglucose and abbreviated [18
F
]FDG, 2-[18
F
]FDG
or FDG, is a radiopharmaceutical, specifically a radiotracer, used in the medical imaging modality positron emission tomography (PET). Chemically, it is 2-deoxy-2-[18
F
]fluoro-D-glucose
, a glucose analog, with the positron-emitting radionuclide fluorine-18 substituted for the normal hydroxyl group at the C-2 position in the glucose molecule.

The uptake of [18
F
]FDG by tissues is a marker for the tissue uptake of glucose, which in turn is closely correlated with certain types of tissue metabolism. After [18
F
]FDG is injected into a patient, a PET scanner can form two-dimensional or three-dimensional images of the distribution of [18
F
]FDG within the body.

Since its development in 1976, [18
F
]FDG has had a profound influence on research in the neurosciences. The subsequent discovery in 1980 that [18
F
]FDG accumulates in tumors underpins the evolution of PET as a major clinical tool in cancer diagnosis. [18
F
]FDG is now the standard radiotracer used for PET neuroimaging and cancer patient management.

The images can be assessed by a nuclear medicine physician or radiologist to provide diagnoses of various medical conditions.

In 1968, Dr. Josef Pacák, Zdeněk Točík and Miloslav Černý at the Department of Organic Chemistry, Charles University, Czechoslovakia were the first to describe the synthesis of FDG. Later, in the 1970s, Tatsuo Ido and Al Wolf at the Brookhaven National Laboratory were the first to describe the synthesis of FDG labeled with fluorine-18. The compound was first administered to two human volunteers by Abass Alavi in August 1976 at the University of Pennsylvania. Brain images obtained with an ordinary (non-PET) nuclear scanner demonstrated the concentration of [18F]FDG in that organ (see history reference below).

Beginning in August 1990, and continuing throughout 1991, a shortage of oxygen-18, a raw material for FDG, made it necessary to ration isotope supplies. Israel's oxygen-18 facility had shut down due to the Gulf War, and the U.S. government had shut down its isotopes of carbon, oxygen and nitrogen facility at Los Alamos National Laboratory, leaving Isotec as the main supplier.

[18F]FDG was first synthesized via electrophilic fluorination with [18F]F2. Subsequently, a "nucleophilic synthesis" was devised with the same radioisotope.

As with all radioactive 18F-labeled radioligands, the fluorine-18 must be made initially as the fluoride anion in a cyclotron. Synthesis of complete [18F]FDG radioactive tracer begins with synthesis of the unattached fluoride radiotracer, since cyclotron bombardment destroys organic molecules of the type usually used for ligands, and in particular, would destroy glucose.

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