TSPO PET using 18F-GE-180: a new perspective in neurooncology?

Langen, Karl‐Josef; Willuweit, Antje

doi:10.1007/s00259-017-3838-6

“…TSPO is overexpressed in activated microglia and macrophages, but also in glioma cells [46]. PET imaging of gliomas using TSPO ligands depicts tumours with high contrast compared with the normal brain [47], but discrimination between tumour mass and brain tissue appears to be critical at the tumour rim, where glia-associated microglia/macrophages may also show high tracer binding [48][49][50]. TSPO ligands accumulate in brain areas with intact BBB, but differences exist in the visualisation of tumour extent compared with amino acid PET [51].…”

Section: Pet Tracers For Brain Tumour Imagingmentioning

confidence: 99%

Hybrid PET/MRI in Cerebral Glioma: Current Status and Perspectives

Langen

¹

,

Galldiks

²

,

Mauler

³

et al. 2023

Cancers

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Advanced MRI methods and PET using radiolabelled amino acids provide valuable information, in addition to conventional MR imaging, for brain tumour diagnostics. These methods are particularly helpful in challenging situations such as the differentiation of malignant processes from benign lesions, the identification of non-enhancing glioma subregions, the differentiation of tumour progression from treatment-related changes, and the early assessment of responses to anticancer therapy. The debate over which of the methods is preferable in which situation is ongoing, and has been addressed in numerous studies. Currently, most radiology and nuclear medicine departments perform these examinations independently of each other, leading to multiple examinations for the patient. The advent of hybrid PET/MRI allowed a convergence of the methods, but to date simultaneous imaging has reached little relevance in clinical neuro-oncology. This is partly due to the limited availability of hybrid PET/MRI scanners, but is also due to the fact that PET is a second-line examination in brain tumours. PET is only required in equivocal situations, and the spatial co-registration of PET examinations of the brain to previous MRI is possible without disadvantage. A key factor for the benefit of PET/MRI in neuro-oncology is a multimodal approach that provides decisive improvements in the diagnostics of brain tumours compared with a single modality. This review focuses on studies investigating the diagnostic value of combined amino acid PET and ‘advanced’ MRI in patients with cerebral gliomas. Available studies suggest that the combination of amino acid PET and advanced MRI improves grading and the histomolecular characterisation of newly diagnosed tumours. Few data are available concerning the delineation of tumour extent. A clear additive diagnostic value of amino acid PET and advanced MRI can be achieved regarding the differentiation of tumour recurrence from treatment-related changes. Here, the PET-guided evaluation of advanced MR methods seems to be helpful. In summary, there is growing evidence that a multimodal approach can achieve decisive improvements in the diagnostics of cerebral gliomas, for which hybrid PET/MRI offers optimal conditions.

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“…The first-generated tracer 11 C-PK11195 has several disadvantages such as limited brain entrance, poor signal-to-noise ratio, and labeling with the impractically rapidly decaying isotope that affects the specificity of TSPO detection [ 63 ]. Novel radiotracers have improved the ability to measure TSPO in vivo [ 64 ]. The second-generated tracers, such as 18 F-DPA-714, 11 C-PBR28, and 18 F-PBR111, with better enhanced pharmacological and pharmacokinetic properties, offer more appropriate tools for in vivo TSPO-PET imaging [ 52 ].…”

Section: Brain Imaging Markersmentioning

confidence: 99%

“…Behavioural Neurology radiotracers have improved the ability to measure TSPO in vivo [64]. The second-generated tracers, such as 18 F-DPA-714, 11 C-PBR28, and 18 F-PBR111, with better enhanced pharmacological and pharmacokinetic properties, offer more appropriate tools for in vivo TSPO-PET imaging [52].…”

Section: Brain Imaging Markersmentioning

confidence: 99%

Advances regarding Neuroinflammation Biomarkers with Noninvasive Techniques in Epilepsy

Ma

¹

,

Hua

²

2021

Behavioural Neurology

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A rapidly growing body of evidence supports that neuroinflammation plays a major role in epileptogenesis and disease progression. The capacity to identify pathological neuroinflammation in individuals with epilepsy is a crucial step on the timing of anti-inflammatory intervention and patient selection, which will be challenging aspects in future clinical studies. The discovery of noninvasive biomarkers that are accessible in the blood or molecular neuroimaging would facilitate clinical translation of experimental findings into humans. These innovative and noninvasive approaches have the advantage of monitoring the dynamic changes of neuroinflammation in epilepsy. Here, we will review the available evidence for the measurement of neuroinflammation in patients with epilepsy using noninvasive techniques and critically analyze the major scientific challenges of noninvasive methods. Finally, we propose the potential for use in clinical applications.

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“…Therefore, several secondgeneration 18 F-labelled TSPO PET ligands, including [ 18 F]FEPPA [40][41][42][43], [ 18 F]FEDAA1106 [44,45], [ 18 F]DPA-714 [46,47], and [ 18 F]PBR06 [48,49] have been developed (for review, see [50,51]). Recently, a novel thirdgeneration TSPO PET ligand, [ 18 F]GE180 was developed [52][53][54] and proved to be useful for TSPO imaging [53,55,56]. However, its application for neuroimaging is very limited as it suffers from very low brain penetration, similar to that of [ 11 C]PK-11195.…”

Section: Introductionmentioning

confidence: 99%

Neuroinflammation in Low-Level PM2.5-Exposed Rats Illustrated by PET via an Improved Automated Produced [¹⁸F]FEPPA: A Feasibility Study

Cheng

¹

,

Cheng

²

,

Guo

³

et al. 2022

Mol Imaging

1

0

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Background. [18F]FEPPA is a potent TSPO imaging agent that has been found to be a potential tracer for imaging neuroinflammation. In order to fulfill the demand of this tracer for preclinical and clinical studies, we have developed a one-pot automated synthesis with simplified HPLC purification of this tracer, which was then used for PET imaging of neuroinflammation in fine particulate matter- (PM2.5-) exposed rats. Results. Using this automated synthesis method, the RCY of the [18F]FEPPA was 38 ± 4 % ( n = 17 , EOB) in a synthesis time of 83 ± 8 min from EOB. The radiochemical purity and molar activities were greater than 99% and 209 ± 138 GBq/μmol (EOS, n = 15 ), respectively. The quality of the [18F]FEPPA synthesized by this method met the U.S. Pharmacopoeia (USP) criteria. The stability test showed that the [18F]FEPPA was stable at 21 ± 2 °C for up to 4 hr after the end of synthesis (EOS). Moreover, microPET imaging showed that increased tracer activity of [18F]FEPPA in the brain of PM2.5-exposed rats ( n = 6 ) were higher than that of normal controls ( n = 6 ) and regional-specific. Conclusions. Using the improved semipreparative HPLC purification, [18F]FEPPA has been produced in high quantity, high quality, and high reproducibility and, for the first time, used for PET imaging the effects of PM2.5 in the rat brain. It is ready to be used for imaging inflammation in various clinical or preclinical studies, especially for nearby PET centers without cyclotrons.

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TSPO PET using 18F-GE-180: a new perspective in neurooncology?

Cited by 6 publications

References 17 publications

Hybrid PET/MRI in Cerebral Glioma: Current Status and Perspectives

Hybrid PET/MRI in Cerebral Glioma: Current Status and Perspectives

Advances regarding Neuroinflammation Biomarkers with Noninvasive Techniques in Epilepsy

Neuroinflammation in Low-Level PM2.5-Exposed Rats Illustrated by PET via an Improved Automated Produced [¹⁸F]FEPPA: A Feasibility Study

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TSPO PET using 18F-GE-180: a new perspective in neurooncology?

Cited by 6 publications

References 17 publications

Hybrid PET/MRI in Cerebral Glioma: Current Status and Perspectives

Hybrid PET/MRI in Cerebral Glioma: Current Status and Perspectives

Advances regarding Neuroinflammation Biomarkers with Noninvasive Techniques in Epilepsy

Neuroinflammation in Low-Level PM2.5-Exposed Rats Illustrated by PET via an Improved Automated Produced [18F]FEPPA: A Feasibility Study

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Product

Resources

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Neuroinflammation in Low-Level PM2.5-Exposed Rats Illustrated by PET via an Improved Automated Produced [¹⁸F]FEPPA: A Feasibility Study