Hypoxia has been observed in a variety of human tumor types and evaluating tumor hypoxia is important because it increases
resistance to radiotherapy and chemotherapy by inducing proteomic change that allow the tumor cell to survive in their hypoxic
environment. One of the major proteomic changes is HIF-1 expression, and HIF-1 has become a target for anti-cancer drugs development
because of its central role in hypoxia-mediated aggressiveness of tumor cells and their resistance to therapy.
Since tumor hypoxia is a key mechanism that leads to resistance of treatment, a large number of challenges for hypoxia imaging
including magnetic resonance, optical, and nuclear imaging have been reported. These hypoxia imaging techniques may have potential in
selecting cancer patients who would benefit from treatments that overcome the presence of hypoxia. Hypoxia imaging could also be used
to document whether or not and the extent to which reoxygenation of tumors occurs during cancer treatment. One of key requirements of
ideal method for imaging hypoxia is that the method should be non-invasive. From an imaging perspective, PET is also one of leading
tools for imaging hypoxia because of its high spatial resolution, high sensitivity, and advantages for visualizing molecular events in living
human tissue. In this review, PET-based radiopharmaceuticals including 18F-FMISO, 18F-FETNIM, 18F-FAZA, and radioactive Cu-
ATSM were summarized from published studies about radiosyntheses, pre-clinical data, and clinical data, which are the lead contenders
for human application.
Keywords: Cu-ATSM, 18F-FAZA, 18F-FETNIM, 18F-FMISO, Hypoxia, PET, human tumor, radiotherapy, chemotherapy, proteomic
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