Synthesis of 2′-fluoro-5-[11C]-methyl-1-β-d-arabinofuranosyluracil ([11C]-FMAU): A potential nucleoside analog for in vivo study of cellular proliferation with PET
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Tracking Docetaxel-Induced Cellular Proliferation Changes in Prostate Tumor-Bearing Mice with <sup>18</sup>F-FMAU PET
2023, Academic RadiologyCitation Excerpt :Preliminary pharmacokinetic studies by others and by us have shown that radiolabeled FMAU behaves very similar to thymidine with respect to the rate of cellular uptake, saturability of cellular incorporation, and presence of intracellular metabolite pools. Radioisotopes carried by FMAU are resistant to degradation and are selectively retained in DNA, reflective of tumor cell division (10–12). Currently, several clinical trials (NCT02809690 and NCT02079181) are underway to investigate the utility of 18F-FMAU in diagnosing and characterizing cancers, including prostate cancer, breast cancer, and brain cancer.
Microwave-assisted one-pot radiosynthesis of 2'-deoxy-2'-[<sup>18</sup>F]fluoro-5-methyl-1-β-d-arabinofuranosyluracil ([<sup>18</sup>F]-FMAU)
2012, Nuclear Medicine and BiologyCitation Excerpt :Further clinical investigation of C-11 or F-18 radiolabeled FMAU, in comparison with [18F]-FLT, is warranted, which may ultimately complement the role of [18F]-FLT or other cell proliferation markers currently under development. The radiosynthesis of [11C]-FMAU was first reported in our group [5]. However, the procedure to prepare [11C]-FMAU involves the formation of dilithio compound which makes the production complicated, hard to control, and unreliable.
The improved syntheses of 5-substituted 2'-[<sup>18</sup>F]fluoro-2'-deoxy-arabinofuranosyluracil derivatives ([<sup>18</sup>F]FAU, [<sup>18</sup>F]FEAU, [<sup>18</sup>F]FFAU, [<sup>18</sup>F]FCAU, [<sup>18</sup>F]FBAU and [<sup>18</sup>F]FIAU) using a multistep one-pot strategy
2011, Nuclear Medicine and BiologyPositron emission tomography imaging of cancer biology: Current status and future prospects
2011, Seminars in OncologyCitation Excerpt :Moreover, high physiological uptake of [18F]FLT in bone marrow and liver will pose a problem in the assessment of therapy response of disease involving these organs. FMAU has been developed for cell proliferation imaging with labeling either in the 5-methyl group of the pyrimidine base with 11C or at the 2′-fluoro position of the sugar with 18F.101 Preclinical studies have shown that FMAU retention in tumors and nontumor tissues with rapid cell turnover (eg, marrow and small intestine) reflects incorporation into DNA.102,103
Molecular Imaging and Targeted Therapy: Radiopharmaceuticals and Clinical Applications, Second Edition
2023, Molecular Imaging and Targeted Therapy: Radiopharmaceuticals and Clinical Applications, Second Edition