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

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 Ge-68/Ga-68 generators. Recently, there has been significant progress in the preparation of novel Ga-68-labeled complexes bearing nitroimidazole moieties for the diagnosis of hypoxia. This review provides a comprehensive overview of the current status of developing Ga-68-labeled radiopharmaceuticals with nitroimidazole moieties, their pharmacokinetics, and in vitro and in vivo studies, as well as PET imaging studies for hypoxic tumors.

Automated summary

Positron emission tomography (PET) is a noninvasive molecular imaging method widely used in the detection and treatment of various diseases. Hypoxia, a common phenomenon in solid tumors, can be detected using radiopharmaceuticals containing nitroimidazole. Gallium-68, a positron-emitting radioisotope, has been developed as a convenient radiotracer for PET imaging of hypoxic tumors. This review provides a comprehensive overview of the development of Ga-68-labeled radiopharmaceuticals with nitroimidazole moieties for the diagnosis of hypoxia.