Preclinical evaluation and validation of [18F]HX4, a promising hypoxia marker for PET imaging

Proc Natl Acad Sci U S A. 2011 Aug 30;108(35):14620-5. doi: 10.1073/pnas.1102526108. Epub 2011 Aug 23.

Abstract

Hypoxia has been shown to be an important microenvironmental parameter influencing tumor progression and treatment efficacy. Patient guidance for hypoxia-targeted therapy requires evaluation of tumor oxygenation, preferably in a noninvasive manner. The aim of this study was to evaluate and validate the uptake of [(18)F]HX4, a novel developed hypoxia marker for PET imaging. A heterogeneous accumulation of [(18)F]HX4 was found within rat rhabdomyosarcoma tumors that was significantly (P < 0.0001) higher compared with the surrounding tissues, with temporal increasing tumor-to-blood ratios reaching a plateau of 7.638 ± 0.926 and optimal imaging properties 4 h after injection. [(18)F]HX4 retention in normal tissues was found to be short-lived, homogeneous and characterized by a fast progressive temporal clearance. Heterogeneity in [(18)F]HX4 tumor uptake was analyzed based on 16 regions within the tumor according to the different orthogonal planes at the largest diameter. Validation of heterogeneous [(18)F]HX4 tumor uptake was shown by a strong and significant relationship (r = 0.722; P < 0.0001) with the hypoxic fraction as calculated by the percentage pimonidazole-positive pixels. Furthermore, a causal relationship with tumor oxygenation was established, because combination treatment of nicotinamide and carbogen resulted in a 40% reduction (P < 0.001) in [(18)F]HX4 tumor accumulation whereas treatment with 7% oxygen breathing resulted in a 30% increased uptake (P < 0.05). [(18)F]HX4 is therefore a promising candidate for noninvasive detection and evaluation of tumor hypoxia at a macroscopic level.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biomarkers
  • Cell Hypoxia*
  • Fluorine Radioisotopes*
  • Imidazoles*
  • Male
  • Neoplasms, Experimental / metabolism*
  • Nitroimidazoles / pharmacology
  • Positron-Emission Tomography / methods*
  • Radiopharmaceuticals*
  • Rats
  • Triazoles*

Substances

  • Biomarkers
  • Fluorine Radioisotopes
  • HX4 compound
  • Imidazoles
  • Nitroimidazoles
  • Radiopharmaceuticals
  • Triazoles
  • pimonidazole