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Open AccessReview

Approaches to PET Imaging of Glioblastoma

by Lindsey R. Drake 1,2,*, Ansel T. Hillmer 1,2,3,4 and Zhengxin Cai 1,2
Yale PET Center, Yale University School of Medicine, New Haven, CT 06511, USA
Department of Radiology and Bioimaging Sciences, Yale University School of Medicine, New Haven, CT 06511, USA
Department of Psychiatry, Yale University School of Medicine, New Haven, CT 06511, USA
Department of Biomedical Engineering, Yale School of Engineering and Applied Science, New Haven, CT 06511, USA
Author to whom correspondence should be addressed.
Academic Editor: Peter Brust
Molecules 2020, 25(3), 568;
Received: 11 December 2019 / Revised: 22 January 2020 / Accepted: 23 January 2020 / Published: 28 January 2020
(This article belongs to the Special Issue Radiolabelled Molecules for Brain Imaging with PET and SPECT)
Glioblastoma multiforme (GBM) is the deadliest type of brain tumor, affecting approximately three in 100,000 adults annually. Positron emission tomography (PET) imaging provides an important non-invasive method of measuring biochemically specific targets at GBM lesions. These powerful data can characterize tumors, predict treatment effectiveness, and monitor treatment. This review will discuss the PET imaging agents that have already been evaluated in GBM patients so far, and new imaging targets with promise for future use. Previously used PET imaging agents include the tracers for markers of proliferation ([11C]methionine; [18F]fluoro-ethyl-L-tyrosine, [18F]Fluorodopa, [18F]fluoro-thymidine, and [18F]clofarabine), hypoxia sensing ([18F]FMISO, [18F]FET-NIM, [18F]EF5, [18F]HX4, and [64Cu]ATSM), and ligands for inflammation. As cancer therapeutics evolve toward personalized medicine and therapies centered on tumor biomarkers, the development of complimentary selective PET agents can dramatically enhance these efforts. Newer biomarkers for GBM PET imaging are discussed, with some already in use for PET imaging other cancers and neurological disorders. These targets include Sigma 1, Sigma 2, programmed death ligand 1, poly-ADP-ribose polymerase, and isocitrate dehydrogenase. For GBM, these imaging agents come with additional considerations such as blood–brain barrier penetration, quantitative modeling approaches, and nonspecific binding. View Full-Text
Keywords: PET imaging; GBM; biomarkers; Sigma 1; Sigma 2; PD-L1; PARP; IDH PET imaging; GBM; biomarkers; Sigma 1; Sigma 2; PD-L1; PARP; IDH
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Drake, L.R.; Hillmer, A.T.; Cai, Z. Approaches to PET Imaging of Glioblastoma. Molecules 2020, 25, 568.

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