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Review

3'-Deoxy-3'-[18F]fluorothymidine

Kam Leung  1
In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004.
[updated ].
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Review

3'-Deoxy-3'-[18F]fluorothymidine

Kam Leung.
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Excerpt

One of the characteristics of tumor cells is their unchecked proliferation. It is important to measure the proliferation rate of cancer lesions to help differentiate benign from malignant tumors and to characterize malignant tumors among normal tissues. 2-[18F]Fluoro-2-deoxy-D-glucose ([18F]FDG) has been widely used in cancer imaging. However, enhanced uptakes of FDG also occur in inflammatory cells and lesions as well as in necrotic cells (1, 2). Thymidine (TdR) and TdR analogs are the standard markers for DNA synthesis, and [11C]thymidine has been used in positron emission tomography (PET) imaging to measure tumor growth rate in situ. Because of the short half-life of 11C and extensive metabolism of [11C]TdR in the blood (3), 3'-deoxy-3'-[18F]fluorothymidine (FLT) was developed for PET imaging.

FLT is an analog of TdR and is phosphorylated by thymidine kinase-1 (TK-1), an enzyme expressed during the DNA synthesis phase of the cell cycle (4). Most cancer cells have a much higher TK-1 activity than normal cells. FLT monophosphate is not incorporated into DNA and is impermeable to the cell membrane. Therefore, it is metabolically trapped inside the cells. The uptake and accumulation of FLT are used as an index of cellular proliferation. [18F]FLT PET has been used to detect and monitor tumor proliferation, to evaluate the stages of tumor, and to detect metastases (5).

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