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Review
. 2023 Jun 23;24(13):10552.
doi: 10.3390/ijms241310552.

Recent Advances of 68Ga-Labeled PET Radiotracers with Nitroimidazole in the Diagnosis of Hypoxia Tumors

Anh Thu Nguyen  1   2 , Hee-Kwon Kim  1   2
Affiliations
Review

Recent Advances of 68Ga-Labeled PET Radiotracers with Nitroimidazole in the Diagnosis of Hypoxia Tumors

Anh Thu Nguyen et al. Int J Mol Sci. .

Abstract

Positron emission tomography (PET) is a noninvasive molecular imaging method extensively applied in the detection and treatment of various diseases. Hypoxia is a common phenomenon found in most solid tumors. Nitroimidazole is a group of bioreducible pharmacophores that selectively accumulate in hypoxic regions of the body. Over the past few decades, many scientists have reported the use of radiopharmaceuticals containing nitroimidazole for the detection of hypoxic tumors. Gallium-68, a positron-emitting radioisotope, has a favorable half-life time of 68 min and can be conveniently produced by 68Ge/68Ga generators. Recently, there has been significant progress in the preparation of novel 68Ga-labeled complexes bearing nitroimidazole moieties for the diagnosis of hypoxia. This review provides a comprehensive overview of the current status of developing 68Ga-labeled radiopharmaceuticals with nitroimidazole moieties, their pharmacokinetics, and in vitro and in vivo studies, as well as PET imaging studies for hypoxic tumors.

Keywords: Ga-68; PET; hypoxia; radiopharmaceuticals; tumor.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Diagram of PET study with 68Ga-labeled radiotracer in hypoxic tumor.
Scheme 1
Scheme 1
Synthesis of 67Ga-DOTA-MN2.
Scheme 2
Scheme 2
Syntheses of 68Ga-NOTA-NI and 68Ga-SCN-NOTA-NI.
Scheme 3
Scheme 3
Syntheses of [68Ga]12 and [68Ga]13.
Scheme 4
Scheme 4
Syntheses of [68Ga]17 and [68Ga]18.
Scheme 5
Scheme 5
Syntheses of [67/68Ga]22 and [67Ga]23.
Scheme 6
Scheme 6
Syntheses of [68Ga]28, [68Ga]29, [68Ga]30, and [68Ga]31.
Scheme 7
Scheme 7
Syntheses of [67/68Ga]47–55.
Scheme 8
Scheme 8
Synthesis of 68Ga-HP-DO3A-NI ([68Ga]58).
Scheme 9
Scheme 9
Syntheses of [68Ga]66–71.
Scheme 10
Scheme 10
Syntheses of [68Ga]75 and [68Ga]76.
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