ArticleMolecular imaging and biology2012
Tracer level electrophilic synthesis and pharmacokinetics of the hypoxia tracer [(18)F]EF5.
Article in Molecular imaging and biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 20 citations in OpenAlex.
- Repeatability of tumour hypoxia imaging using [European journal of nuclear medicine and molecular imaging · 2018Trial
- Closing the gap betweenEJNMMI radiopharmacy and chemistry · 2021Review
- The feasibility of [EJNMMI research · 2020Article
- Prognostic value of tumour blood flow, [¹⁸F]EF5 and [¹⁸F]FDG PET/CT imaging in patients with head and neck cancer treated with radiochemotherapy.European journal of nuclear medicine and molecular imaging · 2014Article
- Comparison of the Hypoxia PET Tracer (18)F-EF5 to Immunohistochemical Marker EF5 in 3 Different Human Tumor Xenograft Models.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2014Article
- Uptake of [Translational oncology · 2014Article
- Evaluation of repeated [(18)F]EF5 PET/CT scans and tumor growth rate in experimental head and neck carcinomas.EJNMMI research · 2014Article
- Imaging hypoxia to improve radiotherapy outcome.Nature reviews. Clinical oncology · 2012Review
- A simplified synthesis of the hypoxia imaging agent 2-(2-Nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-[(18)F]pentafluoropropyl)-acetamide ([18F]EF5).Nuclear medicine and biology · 2012Article
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10 authors at 4 institutions in 2 countries.
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No grant is acknowledged in the PubMed record.
Abstract
purpose2-(2-nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl)-acetamide labeled with [(18)F]-fluorine ([(18)F]EF5), a promising tracer for tumor hypoxia, has previously been synthesized in low yields and low specific radioactivity. In pharmacokinetic evaluations, in the presence of non-radioactive EF5, a uniform and low background uptake and high in vivo stability of [(18)F]EF5 have been demonstrated. Our purpose was to increase the specific radioactivity of [(18)F]EF5 to enable to study the pharmacokinetics at trace level. PROCEDURES: [(18)F]EF5 was synthesized using high specific radioactivity electrophilic [(18)F]F(2) as labelling reagent. Biodistribution of [(18)F]EF5 was determined in a prostate tumor mouse model, and formation of radiolabelled metabolites was studied in mouse, rat and human plasma.
resultsOn average, 595 ± 153 MBq of [(18)F]EF5 was produced. Specific radioactivity was 6.6 ± 1.9 GBq/μmol and the radiochemical purity exceeded 99.0%. [(18)F]EF5 was distributed uniformly in tissues, with highest uptake in liver, kidney, and intestine. Several radiolabelled metabolites were detected in mouse plasma and tissues, whereas low amounts of metabolites were detected in human and rat plasma.
conclusions[(18)F]EF5 was synthesized by electrophilic labelling with high quality and high yields. Pharmacokinetics of [(18)F]EF5 was determined at trace level in several species. Our results suggest that the trace-level approach does not affect the biodistribution of [(18)F]EF5. Extensive metabolism was seen in mouse.
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