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Determination of tumour hypoxia with [(18)F]EF3 in patients with head and neck tumours : a phase I study to assess the tracer pharmacokinetics, biodistribution and metabolism

Bibliographic reference Mahy, Pierre ; Geets, Xavier ; Lonneux, Max ; Levêque, Philippe ; Christian, Nicolas ; et. al. Determination of tumour hypoxia with [(18)F]EF3 in patients with head and neck tumours : a phase I study to assess the tracer pharmacokinetics, biodistribution and metabolism. In: European Journal of Nuclear Medicine and Molecular Imaging, Vol. 35, no. 7, p. 1282-1289 (2008)
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  1. Brizel D, Scully SP, Harrelson JM, Layfield LJ, Bean JM, Prosnitz LR. Tumour oxygenation predicts for the likelihood of distant metastases in human soft tissue sarcoma. Cancer Res. 1996;56:941–3.
  2. Gatenby Robert A., Kessler Howard B., Rosenblum Jay S., Coia Lawrence R., Moldofsky Philip J., Hartz William H., Broder George J., Oxygen distribution in squamous cell carcinoma metastases and its relationship to outcome of radiation therapy, 10.1016/0360-3016(88)90002-8
  3. Hockel M, Schlenger K, Aral B, Mitze M, Schaffer U, Vaupel P. Association between tumour hypoxia and malignant progression in advanced cancer of the uterine cervix. Cancer Res. 1996;56:4509–15.
  4. Stone HB, Brown JM, Phillips TL, Sutherland RM. Oxygen in human tumours: correlations between methods of measurements and response to therapy. Radiat Res. 1993;136:422–34.
  5. Jonathan RA, Wijffels KI, Peeters W, de Wilde PC, Marres HA, Merkx MA, et al. The prognostic value of endogenous hypoxia-related markers for head and neck squamous cell carcinomas treated with ARCON. Radiother Oncol. 2006;79:288–97.
  6. Hodgkiss RJ. Use of 2-nitroimidazoles as bioreductive markers for tumour hypoxia. Anticancer Drug Des. 1998;13:687–702.
  7. Kaanders JHAM, Wijffels KIEM, Marres HAM, Pop LAM, Marres HAM, Ljungkvist ASE, et al. Pimonidazole binding and tumour vascularity predict for treatment outcome in head and neck cancer. Cancer Res. 2002;62:7066–74.
  8. Evans SM, Judy KD, Dunphy I, Jenkins WT, Hwang WT, Nelson PT, et al. Hypoxia is important in the biology and aggression of human glial brain tumours. Clin Cancer Res. 2004;10:8177–84.
  9. Evans Sydney M., Fraker Douglas, Hahn Stephen M., Gleason Kristen, Jenkins W. Timothy, Jenkins Kevin, Hwang Wei-Ting, Zhang Paul, Mick Rosemarie, Koch Cameron J., EF5 binding and clinical outcome in human soft tissue sarcomas, 10.1016/j.ijrobp.2005.05.068
  10. Kaanders JH, Bussink J, van der Kogel AJ. ARCON: a novel biology-based approach in radiotherapy. Lancet Oncol. 2002;3:728–37.
  11. Rischin D, Hicks RJ, Fisher R, Binns D, Corry J, Porceddu S, Trans-Tasman Radiation Oncology Group Study 98.02. Prognostic significance of [18F]-misonidazole positron emission tomography-detected tumor hypoxia in patients with advanced head and neck cancer randomly assigned to chemoradiation with or without tirapazamine: a substudy of Trans-Tasman Radiation Oncology Group Study 98.02. J Clin Oncol. 2006;24:2098–104.
  12. Gregoire V, Haustermans K, Geets X, Roels S, Lonneux M. PET-based treatment planning in radiotherapy: a new standard? J Nucl Med. 2007;48(Suppl 1):68S–77S.
  13. Rajendran JG, Hendrickson KR, Spence AM, Muzi M, Krohn KA, Mankoff DA. Hypoxia imaging-directed radiation treatment planning. Eur J Nucl Med Mol Imaging. 2006;33(Suppl 1):44–53.
  14. Eschmann SM, Paulsen F, Reimold M, Dittmann H, Welz S, Reischl G, et al. Prognostic impact of hypoxia imaging with 18F-misonidazole PET in non-small cell lung cancer and head and neck cancer before radiotherapy. J Nucl Med. 2005;46:253–60.
  15. Mahy P., De Bast M., Leveque P.H., Gillart J., Labar D., Marchand J., Gregoire V., Preclinical validation of the hypoxia tracer 2-(2-nitroimidazol-1-yl)-N-(3,3,3-[18F]trifluoropropyl)acetamide, [18F]EF3, 10.1007/s00259-004-1573-2
  16. Mahy P, De Bast M, Gillart J, Labar D, Grégoire V. Detection of tumour hypoxia: comparison between EF5 adducts and [18F]-EF3 uptake on an individual mouse tumour basis. Eur J Nuc Med Mol Imaging. 2006;33:553–6.
  17. Christian N, Bol A, De Bast M, Labar D, Lee J, Mahy P, et al. Determination of tumour hypoxia with the PET tracer [18F]EF3: improvement of the tumour-to-background ratio in a mouse tumour model. Eur J Nucl Med Mol Imaging. 2007 Sep;34(9):1348–54.
  18. Josse O, Labar D, Georges B, Gregoire V, Marchand-Brynaert J. Synthesis of [18F]-labeled EF3 [2-(2-nitroimidazol-1-yl)-N-(3,3,3-trifluoropropyl)-acetamide], a marker for PET detection of hypoxia. Bioorg Med Chem. 2001;9:665–75.
  19. Lonneux M, Borbath I, Bol A, Coppens A, Sibomana M, Bausart R, et al. Attenuation correction in whole-body FDG oncological studies: the role of statistical reconstruction. Eur J Nucl Med. 1999;26:591–8.
  20. Koch CJ, Hahn SM, Rockwell K Jr, Covey JM, McKenna WG, Evans SM. Pharmacokinetics of EF5 [2-(2-nitro-1-H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl) acetamide] in human patients: implications for hypoxia measurements in vivo by 2-nitroimidazoles. Cancer Chemother Pharmacol. 2001;48:177–87.
  21. Ziemer L., Evans S., Kachur A., Shuman A., Cardi C., Jenkins W., Karp J., Alavi A., Dolbier W., Koch C., Noninvasive imaging of tumor hypoxia in rats using the 2-nitroimidazole 18F-EF5, 10.1007/s00259-002-1037-5
  22. Graham MM, Peterson LM, Link JM, Evans ML, Rasey JS, Koh WJ, et al. Fluorine-18-fluoromisonidazole radiation dosimetry in imaging studies. J Nucl Med. 1997;38:1631–6.
  23. Bruehlmeier M, Roelcke U, Schubiger PA, Ametamey SM. Assessment of hypoxia and perfusion in human brain tumours using PET with 18F-fluoromisonidazole and 15O–H2O. J Nucl Med. 2004;45:1851–9.
  24. Yang D J, Wallace S, Cherif A, Li C, Gretzer M B, Kim E E, Podoloff D A, Development of F-18-labeled fluoroerythronitroimidazole as a PET agent for imaging tumor hypoxia., 10.1148/radiology.194.3.7862981
  25. Koch CJ, Evans SM, Lord EM, Oxygen dependence of cellular uptake of EF5 [2-(2-nitro-1H-imidazol-1-yl)-N-(2,2,3,3,3-pentafluoropropyl)a cet amide]: analysis of drug adducts by fluorescent antibodies vs bound radioactivity, 10.1038/bjc.1995.426
  26. Gronroos T, Eskola O, Lehtio K, Minn H, Marjamaki P, Bergman J, et al. Pharmacokinetics of [18F]FETNIM: a potential marker for PET. J Nucl Med. 2001;42:1397–404.
  27. Lehtio K, Oikonen V, Gronroos T, Eskola O, Kalliokoski K, Bergman J, et al. Imaging of blood flow and hypoxia in head and neck cancer: initial evaluation with [(15)O]H(2)O and [(18)F]fluoroerythronitroimidazole PET. J Nucl Med. 2001;42:1643–52.
  28. Koh Wui-Jin, Rasey Janet S., Evans Margaret L., Grierson John R., Lewellen Thomas K., Graham Michael M., Krohn Kenneth A., Griffin Thomas W., Imaging of hypoxia in human tumors with [F-18]fluoromisonidazole, 10.1016/0360-3016(92)91001-4
  29. Tolvanen T, Lehtio K, Kulmala J, Oikonen V, Eskola O, Bergman J, et al. 18F-Fluoroerythronitroimidazole radiation dosimetry in cancer studies. J Nucl Med. 2002;43:1674–80.
  30. Kumar PD, Stypinski D, Xia H, et al. Fluoroazomycin arabinoside (FAZA): synthesis, 2H and 3H-labelling and preliminary biological evaluation of a novel 2-nitroimidazole marker of tissue hypoxia. J Label Comp Radiopharm. 1999;42:3–16.
  31. Souvatzoglou M, Grosu AL, Röper B, Krause BJ, Beck R, Reischl G, et al. Tumour hypoxia imaging with [18F]FAZA PET in head and neck cancer patients: a pilot study. Eur J Nucl Med Mol Imaging. 2007;34:1566–75.
  32. Seddon BM, Payne GS, Simmons L, Ruddle R, Grimshaw R, Tan S, et al. A phase I study of SR-4554 via intravenous administration for noninvasive investigation of tumour hypoxia by magnetic resonance spectroscopy in patients with malignancy. Clin Cancer Res. 2003;9:5101–12.
  33. Evans SM, Kachur AV, Shiue CA Hustinx R, Jenkins WT, Shive GG, Karp JS, et al. Noninvasive detection of tumour hypoxia using the 2-nitroimidazole [18F]EF1. J Nucl Med. 2000;41:327–36.
  34. Rasey Janet S., Koh Wui-jin, Evans Margaret L., Peterson Lanell M., Lewellen Thomas K., Graham Michael M., Krohn Kenneth A., Quantifying regional hypoxia in human tumors with positron emission tomography of [18F]fluoromisonidazole: A pretherapy study of 37 patients, 10.1016/s0360-3016(96)00325-2
  35. Chapman JD, Zanzocino P. On measuring hypoxia in individual tumours with radiolabeled agents. J Nucl Med. 2001;42:1653–5.
  36. Chapman JD, Engelhardt EL, Stobbe CC, Schneider RF, Hanks GE. Measuring hypoxia and predicting tumour radioresistance with nuclear medicine assays. Radiother Oncol. 1998;46:229–37.
  37. Partridge MA, Spinelli A, Rydera W, Hindorf C. The effect of beta + energy on performance of a small animal PET camera. Nucl Instrum Meth A. 2006;568:933–6.
  38. Riedl CC, Brader P, Zanzonico P, Reid V, Woo Y, Wen B, et al. Tumor hypoxia imaging in orthotopic liver tumors and peritoneal metastasis: a comparative study featuring dynamic (18)F-MISO and (124)I-IAZG PET in the same study cohort. Eur J Nucl Med Mol Imaging. 2008;35:39–46.
  39. Reischl G, Dorow DS, Cullinane C, Katsifis A, Roselt P, Binns D, et al. Imaging of tumor hypoxia with [124I]IAZA in comparison with [18F]FMISO and [18F]FAZA—first small animal PET results. J Pharm Pharm Sci. 2007;10:203–11.
  40. Janssen HL, Haustermans KM, Balm AJ, Begg AC. Hypoxia in head and neck cancer: how much, how important? Head Neck. 2005;27:622–38.