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18F-EF5

EF5 is a nitroimidazole derivative used in oncology research. Due to its similarity in chemical structure to etanidazole, EF5 binds in cells displaying hypoxia.

Non-labeled EF5 has been extensively used in immunohistochemical studies for several years and its hypoxia specificity has been comprehensively evaluated The 18F-radiolabeled derivative of EF5 is being studied for its possibility to be used in positron emission tomography (PET) to detect low levels of oxygen in brain tumors and several other malignant tumors. This can help show how a tumor will respond to treatment.

Targeting tumor hypoxia in cancer treatment aims to overcome radiotherapy resistance of hypoxic tumors. Thus, a major clinical implication for 18F-EF5-PET imaging is expected to be guiding of radiotherapy dose modulation. Clinical studies on 18F-EF5-PET/CT imaging have indicated clinically acceptable biodistribution and dosimetric profile, and in head and neck cancer also favorable imaging characteristics, prognostic value and repeatability. A recent 18F-EF5-PET/MR study showed promising potential in detecting tumor hypoxia in cervical cancer. However, 18F-EF5-PET/CT is not feasible in imaging of ovarian cancer due to physiological intra-abdominal 18F-EF5-accumulation. Further studies evaluating the clinical use of 18F-EF5 PET imaging in head and neck cancer are ongoing.

References

(March 2006). "EF5 binding and clinical outcome in human soft tissue sarcomas". International Journal of Radiation Oncology, Biology, Physics.
(December 1993). "Detection of hypoxic cells by monoclonal antibody recognizing 2-nitroimidazole adducts". Cancer Research.
(March 2015). "Optimizing hypoxia detection and treatment strategies". Seminars in Nuclear Medicine.
(2002). "Measurement of absolute oxygen levels in cells and tissues using oxygen sensors and 2-nitroimidazole EF5". Elsevier.
(February 2003). "Noninvasive imaging of tumor hypoxia in rats using the 2-nitroimidazole 18F-EF5". European Journal of Nuclear Medicine and Molecular Imaging.
(September 2012). "Radiation dosimetry and biodistribution of the hypoxia tracer (18)F-EF5 in oncologic patients". Cancer Biotherapy & Radiopharmaceuticals.
(December 2008). "18F-EF5: a new PET tracer for imaging hypoxia in head and neck cancer". Journal of Nuclear Medicine.
(November 2014). "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.
(February 2018). "Repeatability of tumour hypoxia imaging using [¹⁸F]EF5 PET/CT in head and neck cancer". European Journal of Nuclear Medicine and Molecular Imaging.
(December 2021). "Imaging of Tumor Hypoxia With 18F-EF5 PET/MRI in Cervical Cancer". Clinical Nuclear Medicine.
(September 2020). "The feasibility of [¹⁸F]EF5-PET/CT to image hypoxia in ovarian tumors: a clinical study". EJNMMI Research.

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diagnostic-medical-imaging nitroimidazoles

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