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Early Clinical PET Imaging Results with the Novel PHF-Tau Radioligand [F-18]-T807
Abstract
Aggregates of hyperphosphorylated tau (PHF-tau), such as neurofibrillary tangles, are linked to the degree of cognitive impairment in Alzheimer's disease. We have developed a novel PHF-tau targeting positron emission tomography imaging agent, [F-18]-T807, which may be useful for imaging Alzheimer's disease and other tauopathies. Here in, we describe the first human brain images with [F-18]-T807.
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In the citing paper
“However, at least one first-generation ligand has emerged as a reliable biomarker of 3R/4R PHF tau deposits [28].”
From NIA‐AA Research Framework: Toward a biological definition of Alzheimer's disease (2018) · cites this paper as [28]
In the citing paper
“18F-AV-1451 was originally developed to bind to paired helical filament tau in Alzheimer’s disease (Zhang et al., 2012; Chien et al., 2013; Xia et al., 2013), and has been extensively used in Alzheimer’s and non-Alzheimer’s diseases.”
From Neuroinflammation and protein aggregation co-localize across the frontotemporal dementia spectrum (2020) · cites this paper as Chien et al., 2013
In the citing paper
“Imaging biomarkers for cortical tau have become available.19,20”
From Positron Emission Tomography Imaging With [ 18 F]flortaucipir and Postmortem Assessment of Alzheimer Disease Neuropathologic Changes (2020) · cites this paper as [19]
In the citing paper
“Flortaucipir is being developed as a PET tracer for detection of the aggregated tau of AD.19,21,22,23,24”
From Positron Emission Tomography Imaging With [ 18 F]flortaucipir and Postmortem Assessment of Alzheimer Disease Neuropathologic Changes (2020) · cites this paper as [19]
In the citing paper
“As expected, in vitro QC-01–175 and T807 displayed a significantly lower affinity for all recombinant immobilized tau forms than the reported KD of T807 for native, aggregated tau filaments from AD brain sections (KD15 nM)”
From Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models (2019) · cites this paper as Chien et al., 2013
In the citing paper
“However, small-molecule probes against tau oligomeric species, such as 18F-T807, have been developed and are currently in use as clinical tau PET tracers190.”
From PROTAC targeted protein degraders: the past is prologue (2022) · cites this paper as [190]
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Items 301–400 of 653
Invited review: Drug development for tauopathies
Grüninger, F. (2014) · Neuropathology and Applied Neurobiology · doi:10.1111/nan.12192 · Cited by 40
Relationships between β-amyloid and tau in an elderly population: An accelerated failure time model
Therneau, T. M., Knopman, D. S., Lowe, V. J., Botha, H., Graff‐Radford, J., Jones, D. T., Vemuri, P., Mielke, M. M., Schwarz, C. G., Senjem, M. L., et al. (2021) · NeuroImage · doi:10.1016/j.neuroimage.2021.118440 · Cited by 36
“, 2004) and tau PET with flortaucipir (Chien et al., 2013) on either GE or Siemens scanners.”
Shimojo, M., Higuchi, M., Suhara, T., & Sahara, N. (2015) · Frontiers in Neuroscience · doi:10.3389/fnins.2015.00482 · Cited by 37
Clinical Applications of Small-molecule PET Radiotracers: Current Progress and Future Outlook
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Emerging Diagnostic and Therapeutic Strategies for Tauopathies
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“neurodegenerative disorders and even entered clinical trials [20-25].”
BackgroundInfluentialWhitwell, J. L., Ahlskog, J. E., Tosakulwong, N., Senjem, M. L., Spychalla, A. J., Petersen, R. C., Jack, C. R., Lowe, V. J., & Josephs, K. A. (2017) · Parkinsonism & Related Disorders · doi:10.1016/j.parkreldis.2017.12.016 · Cited by 40
“Thirty subjects with probable PSP had been recruited into an NIH-funded study (Co-PI’s Josephs/Whitwell) and underwent [18F]AV-1451 PET imaging to assess tau[7, 21], Pittsburgh Compound B (PiB) PET to assess beta-amyloid deposition and a volumetric MRI.”
MethodPET Agents in Dementia: An Overview
van Waarde, A., Marcolini, S., Deyn, P. P. D., & Dierckx, R. (2021) · Seminars in Nuclear Medicine · doi:10.1053/j.semnuclmed.2020.12.008 · Cited by 39
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“Flortaucipir uptake does not reach equilibrium, with tissues showing uptake-dependent rising SUVr values over time [40, 41].”
[ 18 F]Flortaucipir PET Across Various MAPT Mutations in Presymptomatic and Symptomatic Carriers
Wolters, E. E., Papma, J. M., Verfaillie, S. C. J., Visser, D., Weltings, E., Groot, C., van der Ende, E. L., Giannini, L. A. A., Tuncel, H., Timmers, T., et al. (2021) · Neurology · doi:10.1212/wnl.0000000000012448 · Cited by 37
Tau Positron Emission Tomography ImagingPreprint
Kolb, H. C., & Andrés, J. I. (2016) · Cold Spring Harbor Perspectives in Biology · doi:10.1101/cshperspect.a023721 · Cited by 37
“In vitro autoradiography staining of human AD brain sections revealed that the distribution of THK-5105 and THK-5117 in the mesial temporal sections coincided with Gallyas–Braak staining and tau immunostaining but not with the distribution of Pittsburgh compound B (PiB).”
InfluentialSelf-citationThe Neuropsychiatric Examination of the Young-Onset Dementias
Ducharme, S., & Dickerson, B. C. (2015) · Psychiatric Clinics of North America · doi:10.1016/j.psc.2015.01.002 · Cited by 39
Quevenco, F. C., Bergen, J. M. G. V., Treyer, V., Studer, S. T., Kagerer, S. M., Meyer, R., Gietl, A. F., Kaufmann, P. A., Nitsch, R. M., Höck, C., et al. (2020) · Frontiers in Aging Neuroscience · doi:10.3389/fnagi.2020.00046 · Cited by 34
“The current study also included measures of tau load, by assessing local retention of 18F-AV1451 using an established PET procedure (Chien et al., 2013).”
MethodHsu, J., Lin, K., Hsiao, I., Huang, K., Liu, C., Wu, H.-C., Weng, Y., Huang, C., Chang, C., Yen, T., et al. (2020) · Clinical Nuclear Medicine · doi:10.1097/rlu.0000000000003164 · Cited by 35
Neuroimaging in Alzheimer's Disease for Early Diagnosis: A Comprehensive Review
Aramadaka, S., Mannam, R., Narayanan, R. S., Bansal, A., Yanamaladoddi, V. R., Sarvepalli, S. S., & Vemula, S. L. (2023) · Cureus · doi:10.7759/cureus.38544 · Cited by 46
“18FT808 had a high tau affinity, quick absorption, and clearance, but it had the drawback of defluorination followed by bone uptake [90].”
BackgroundAlzheimer's disease and other dementias: advances in 2013
Reiman, E. M. (2013) · The Lancet Neurology · doi:10.1016/s1474-4422(13)70257-6 · Cited by 36
Rabinovici, G. D., Karlawish, J. H., Knopman, D. S., Snyder, H. M., Sperling, R. A., & Carrillo, M. C. (2016) · Alzheimer s & Dementia · doi:10.1016/j.jalz.2016.03.002 · Cited by 35
Tau PET Imaging with [18F]PM-PBB3 in Frontotemporal Dementia with MAPT Mutation
Su, Y., Fu, J., Yu, J., Zhao, Q., Guan, Y., Zuo, C., Li, M., Tan, H., & Cheng, X. (2020) · Journal of Alzheimer s Disease · doi:10.3233/jad-200287 · Cited by 35
Optimizing Central Nervous System Drug Development Using Molecular Imaging
Hargreaves, R. J., Hoppin, J., Sevigny, J., Patel, S., Chiao, P.-C., Klimas, M. T., & Verma, A. (2015) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.132 · Cited by 34
Tago, T., Furumoto, S., Okamura, N., Harada, R., Adachi, H., Ishikawa, Y., Yanai, K., Iwata, R., & Kudo, Y. (2015) · Molecular Imaging and Biology · doi:10.1007/s11307-015-0879-8 · Cited by 36
Rombouts, F. J. R., Declercq, L., Andrés, J.-I., Bottelbergs, A., Chen, L., Iturrino, L., Leenaerts, J. E., Mariën, J., Song, F., Wintmolders, C., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01759 · Cited by 35
Self-citationFirst Tau PET Tracer Approved: Toward Accurate In Vivo Diagnosis of Alzheimer Disease
Barthel, H. (2020) · Journal of Nuclear Medicine · doi:10.2967/jnumed.120.252411 · Cited by 35
Distinct tau filament folds in human MAPT mutants P301L and P301T
Schweighauser, M., Shi, Y., Murzin, A. G., Garringer, H. J., Vidal, R., Murrell, J. R., Erro, M. E., Seelaar, H., Ferrer, I., Swieten, J. C. V., et al. (2025) · Nature Structural & Molecular Biology · doi:10.1038/s41594-025-01575-9 · Cited by 34
“The observation that the P301L tau folds are different from the folds of wild-type tau may explain why the PET ligand [ 18 F]-flortaucipir, which binds with high affinity to the Alzheimer tau fold, showed only little binding in individuals with the mutation P301L encoded by MAPT 46–49 .”
Synthesis of a PET tau tracer [(11)C]PBB3 for imaging of Alzheimer's disease.
Wang, M., Gao, M., Xu, Z., & Zheng, Q.-H. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.08.053 · Cited by 32
Zhao, Q., Liu, M., Ha, L., Zhou, Y., & Initiative, A. D. N. (2019) · Frontiers in Neurology · doi:10.3389/fneur.2019.00486 · Cited by 39
“n vivo human studies indicated that patterns of 18F-AV1451 retention were paralleled with neuropathological staging of neurofibrillary tau pathology of AD and that tracer retention increased with age even in the presence of cognitive impairment and dementia (18, 20, 21).”
BackgroundThe Role of Tau beyond Alzheimer’s Disease: A Narrative Review
Virgilio, E., Marchi, F. D., Contaldi, E., Dianzani, U., Cantello, R. M., Mazzini, L., & Comi, C. (2022) · Biomedicines · doi:10.3390/biomedicines10040760 · Cited by 32
“The contribution of brain Tau aggregates can be evaluated in vivo using specific radioligands, such as [18F]AV-1451, also known as [18F]T807 [147,148].”
BackgroundAli, F., Whitwell, J. L., Martin, P. R., Senjem, M. L., Knopman, D. S., Jack, C. R., Lowe, V. J., Petersen, R. C., Boeve, B. F., & Josephs, K. A. (2018) · Journal of Neurology · doi:10.1007/s00415-018-8815-x · Cited by 38
Jagust, W. J., Koeppe, R. A., Rabinovici, G. D., Villemagne, V. L., Harrison, T. M., Landau, S. M., & Initiative, T. A. D. N. (2024) · Alzheimer's & Dementia · doi:10.1002/alz.14165 · Cited by 34
“However, the drawback of the approach is that it may reflect overfitting of the specific data set used to define the most sensitive voxels and it thus requires replication.”
Kulichikhin, K. Y., Fedotov, S. A., Rubel, M. S., Zalutskaya, N. M., Zobnina, A. E., Malikova, O. A., Незнанов, Н. Г., Chernoff, Y. O., & Rubel, A. A. (2021) · Prion · doi:10.1080/19336896.2021.1917289 · Cited by 34
“Recently, the method of premortem observation of tangles using PET with (18)F-flortaucipir as the tau-amyloid-specific dye has been developed [38].”
MethodThe role of positron emission tomography imaging in understanding Alzheimer’s disease
Barthel, H., Seibyl, J. P., & Sabri, O. (2015) · Expert Review of Neurotherapeutics · doi:10.1586/14737175.2015.1023296 · Cited by 34
“additional increase in neocortex at later disease stages [61]”
BackgroundTau Imaging in Alzheimer's Disease Diagnosis and Clinical Trials
Brosch, J. R., Farlow, M. R., Risacher, S. L., & Apostolova, L. G. (2016) · Neurotherapeutics · doi:10.1007/s13311-016-0490-y · Cited by 37
“showed uptake in a pattern similar to that predicted by Braak staging in patients with AD [30].”
BackgroundResult[18F]-THK5351 PET Imaging in Patients With Semantic Variant Primary Progressive Aphasia
Lee, H., Seo, S., Lee, S., Jeong, H. J., Woo, S., Lee, K., Lee, Y., Park, K. H., Heo, J., Yoon, C. W., et al. (2017) · Alzheimer Disease & Associated Disorders · doi:10.1097/wad.0000000000000216 · Cited by 35
Synthesis and preliminary evaluation of 2‐arylhydroxyquinoline derivatives for tau imaging
Tago, T., Furumoto, S., Okamura, N., Harada, R., Ishikawa, Y., Arai, H., Yanai, K., Iwata, R., & Kudo, Y. (2013) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.3133 · Cited by 32
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“6–9 The advent of positron emission tomography (PET) imaging ligands that target hyperphosphorylated tau protein (e.g., AV145), 10,11 b -amyloid (e.g. florbetapir, florbetaben, flutemetamol, Pittsburgh compound B) 12–17 and neuroinflammatory processes (e.g., PBR28), 18 may afford the potential to…”
Disease-related patterns of in vivo pathology in Corticobasal syndrome
Initiative, A. D. N., Niccolini, F., Wilson, H., Hirschbichler, S. T., Yousaf, T., Pagano, G., Whittington, A., Caminiti, S. P., Erro, R., Holton, J. L., et al. (2018) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-018-4104-2 · Cited by 35
Yasuno, F., Minami, H., Hattori, H., & Initiative, A. D. N. (2020) · Psychogeriatrics · doi:10.1111/psyg.12552 · Cited by 32
“21 Weighted mean SUVR was calculated from three composite ROIs that correspond to the anatomical de fi nitions of Braak stages 1/2 (ento-rhinal cortex and hippocampus), 3/4 (limbic), and 5/6 (neocortical) with reference to the AV-1451 uptake mean of the inferior cerebellum.”
InfluentialKing‐Robson, J., Initiative, A. D. N., Wilson, H., & Politis, M. (2021) · Journal of Alzheimer s Disease · doi:10.3233/jad-201457 · Cited by 29
Evaluation of [ 18 F]-JNJ-64326067-AAA tau PET tracer in humans
Baker, S. L., Provost, K., Thomas, W., Whitman, A., Janabi, M., Schmidt, M. E., Timmers, M., Kolb, H. C., Rabinovici, G. D., & Jagust, W. J. (2021) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1177/0271678x211031035 · Cited by 33
Self-citationFully automated synthesis of [18F]T807, a PET tau tracer for Alzheimer’s disease
Gao, M., Wang, M., & Zheng, Q. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.05.035 · Cited by 31
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Ono, M., Watanabe, H., Kitada, A., Matsumura, K., Ihara, M., & Saji, H. (2016) · Scientific Reports · doi:10.1038/srep34197 · Cited by 34
18F-AV1451 PET imaging and multimodal MRI changes in progressive supranuclear palsy
Nicastro, N., Rodríguez, P. V., Malpetti, M., Bevan-Jones, W. R., Jones, P. S., Passamonti, L., Aigbirhio, F. I., O'Brien, J. T., & Rowe, J. B. (2019) · Journal of Neurology · doi:10.1007/s00415-019-09566-9 · Cited by 32
Imaging biomarkers in tauopathies
Dani, M., Edison, P., & Brooks, D. J. (2015) · Parkinsonism & Related Disorders · doi:10.1016/j.parkreldis.2015.08.011 · Cited by 29
“M CI cases showed lower uptake than AD patients and uptake correlates with cognitive im pairment [13].”
ResultRiley, D., Robbins, C. A., Cantu, R. C., & Stern, R. A. (2015) · Brain Injury · doi:10.3109/02699052.2014.965215 · Cited by 32
Smith, R. A., Wibom, M., Olsson, T. G., Hägerström, D., Jögi, J., Rabinovici, G. D., & Hansson, O. (2016) · Journal of Alzheimer s Disease · doi:10.3233/jad-151004 · Cited by 30
“We here describe an early-onset, autosomal-dominant AD patient with tau deposition visualized using the newly developed ligand 18 F-AV-1451 (previously named T-807) [4].”
Tudorascu, D., Laymon, C. M., Zammit, M. D., Minhas, D. S., Anderson, S., Ellison, P. A., Zaman, S. H., Ances, B. M., Sabbagh, M. N., Johnson, S., et al. (2020) · Alzheimer s & Dementia Translational Research & Clinical Interventions · doi:10.1002/trc2.12096 · Cited by 30
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“In addition, post-mortem autoradiography followed by immunohistochemistry shows co-localization between these radiopharmaceuticals and phospo-tau antibodies [30,31].”
BackgroundTau in Late-Life Depression: A Systematic Review and Meta-Analysis
Brown, E. E., Iwata, Y., Chung, J. K., Gerretsen, P., & Graff-Guerrero, A. (2016) · Journal of Alzheimer's Disease · doi:10.3233/jad-160401 · Cited by 29
Imaging Brain Metabolism and Pathology in Alzheimer ’s Disease with Positron Emission Tomography
D, R. W. C. (2014) · Journal of Alzheimer’s Disease & Parkinsonism · doi:10.4172/2161-0460.1000143 · Cited by 31
“Chien and colleagues introduced the first human brain images with 18F-T807 [69] and in more recent study with 18F-T808 [70], which showed slower 18F-deflourination and faster pharmacokinetics than 18FT807.”
BackgroundImaging as a biomarker in drug discovery for Alzheimer’s disease: is MRI a suitable technology?
Pich, E. M., Jeromin, A., Frisoni, G. B., Hill, D., Lockhart, A., Schmidt, M. E., Turner, M. R., Mondello, S., & Potter, W. Z. (2014) · Alzheimer s Research & Therapy · doi:10.1186/alzrt276 · Cited by 30
Bai, Y., & Liu, Y. (2021) · Chemistry - A European Journal · doi:10.1002/chem.202102344 · Cited by 30
Multicenter 18F-PI-2620 PET for In Vivo Braak Staging of Tau Pathology in Alzheimer’s Disease
Rullmann, M., Brendel, M., Schroeter, M. L., Saur, D., Levin, J., Perneczky, R. G., Tiepolt, S., Patt, M., Mueller, A., Villemagne, V. L., et al. (2022) · Biomolecules · doi:10.3390/biom12030458 · Cited by 29
“In vivo studies using early-generation tau tracers allowed for the first time to visualize anatomical distribution of tau directly in the living human brain [6,7].”
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Central Nervous System Targeted Protein Degraders
Thomas, B. A. I., Lewis, H. L., Jones, D. H., & Ward, S. E. (2023) · Biomolecules · doi:10.3390/biom13081164 · Cited by 30
“For example, QC-01-175, a Tau-degrading PROTAC based on the PET tracer T807, has been used extensively in vivo to visualise various tauopathies (Figure 6) [40,41].”
BackgroundA closer look at amyloid ligands, and what they tell us about protein aggregates
Chisholm, T. S., & Hunter, C. A. (2023) · Chemical Society Reviews · doi:10.1039/d3cs00518f · Cited by 29
Loftus, J. R., Puri, S., & Meyers, S. P. (2023) · Insights into Imaging · doi:10.1186/s13244-022-01358-6 · Cited by 30
“Currently, the most widely used tau selective radiotracer is older-generation F-18 flortaucipir (Tauvid; Avid Radiopharmaceuticals, previously known as AV 1451 and T807) [65].”
BackgroundMohammadi, Z., Alizadeh, H., Marton, J., & Cumming, P. D. (2023) · Biomolecules · doi:10.3390/biom13020290 · Cited by 28
Gao, M., Wang, M., & Zheng, Q. (2013) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2013.11.025 · Cited by 28
Neuroimaging in the Diagnosis of Chronic Traumatic Encephalopathy: A Systematic Review
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Increased retention of tau PET ligand [18F]-AV1451 in Alzheimer’s Disease Psychosis
Gomar, J. J., Tan, G., Halpern, J. H., Gordon, M. L., GREENWALD, B. S., & Koppel, J. L. (2022) · Translational Psychiatry · doi:10.1038/s41398-022-01850-z · Cited by 27
“Mirroring the relationship between neurofibrillary tangle pathology and clinical disease severity, [(18)F]-AV1451 binding patterns increase in the presence of cognitive impairment and are topographically associated with cortical atrophy and clinical symptomatology [24, 25].”
BackgroundFurr, J. W., Morales‐Scheihing, D., Manwani, B., Lee, J., & McCullough, L. D. (2019) · NeuroMolecular Medicine · doi:10.1007/s12017-019-08568-0 · Cited by 29
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“Much of the published literature 10-28 indicates that the binding of flortaucipir to tau NFTs parallels NFT accumulation described as Braak stages, 10,29-31 especially for A β -positive subjects, 30,32 and correlates with clinical symptoms and measures of neurodegeneration.”
BackgroundThe Effects of Amyloid and Tau on Functional Network Connectivity in Older Populations
Wales, R. M., & Leung, H.-C. (2021) · Brain Connectivity · doi:10.1089/brain.2020.0902 · Cited by 26
“With the recent emergence of the PET tracer, flortau-cipir ( 18 F-AV1451) (Chien et al., 2013), which provides an in vivo visualization of tau distribution in the human brain, the role of tau on brain function has been quickly gaining attention.”
Dynamic nanoassemblies for imaging and therapy of neurological disorders
Zhang, L., Sun, H., Zhao, J., Lee, J., Low, L. E., Gong, L., Chen, Y., Wang, N., Zhu, C., Lin, P., et al. (2021) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2021.113832 · Cited by 27
Dumbbell Aptamer Sensor Based on Dual Biomarkers for Early Detection of Alzheimer’s Disease
Zhou, J., Sun, Y., Zhang, J., Luo, F., Ma, H., Guan, M., Feng, J., & Dong, X. (2023) · ACS Applied Materials & Interfaces · doi:10.1021/acsami.2c21379 · Cited by 26
Role of tau versus TDP‐43 pathology on medial temporal lobe atrophy in aging and Alzheimer's disease
Wisse, L. E. M., Wuestefeld, A., Murray, M. E., Jagust, W. J., & Joie, R. L. (2025) · Alzheimer s & Dementia · doi:10.1002/alz.14582 · Cited by 24
“19 Human biomarker milestones: 1980—first publication of FDG PET in AD 180 ; 1988—first publication of in vivo MRI-based atrophy in AD 1 ; 1995—first publication of A β & tau measures in CSF 181,182 ; 2004—first publication of A β PET 183 ; 2013—first publication of tau PET 184 ; Late 2010s—blood-based biomarker devel…”
InfluentialKey emerging issues in progressive supranuclear palsy and corticobasal degeneration
Josephs, K. A. (2015) · Journal of Neurology · doi:10.1007/s00415-015-7682-y · Cited by 25
“Imaging PET ligands directed at tau are now available [39, 40].”
Drug Development in Alzheimer’s Disease: The Contribution of PET and SPECT
Declercq, L., Vandenberghe, R. R., Laere, K. V., Verbruggen, A., & Bormans, G. M. (2016) · Frontiers in Pharmacology · doi:10.3389/fphar.2016.00088 · Cited by 27
“…first-in-man study on three HCs, in one patient with MCI (MMSE score of 26) and one severe AD patient (MMSE score of 7) in comparison with three HCs. Remarkably, the tracer retention was significantly lower in the patient with MCI, as compared to the patient with severe AD (Chien et al., 2012).”
ResultBeaurain, M., Salabert, A., Ribeiro, M. J., Arlicot, N., Damier, P., Jeune, F. L., Démonet, J., & Payoux, P. (2019) · Frontiers in Medicine · doi:10.3389/fmed.2019.00268 · Cited by 26
“They have a nanomolar affinity for the tau PHF found in AD, and are 25 times more selective for tau PHF than for Aβ (120, 121).”
BackgroundPET and SPECT imaging of the brain: a review on the current status of nuclear medicine in Japan
Kaneta, T. (2020) · Japanese Journal of Radiology · doi:10.1007/s11604-019-00901-8 · Cited by 26
Gong, K., Han, P. K., Johnson, K. A., et al. (2020) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-020-05061-w · Cited by 25
Neuroimaging and traumatic brain injury: State of the field and voids in translational knowledge.
Bruce, E. D., Konda, S., Dean, D., Wang, E. W., Huang, J. H., & Little, D. M. (2015) · Molecular and cellular neurosciences · doi:10.1016/j.mcn.2015.03.017 · Cited by 25
Characterization of the radiolabeled metabolite of tau PET tracer 18F-THK5351
Harada, R., Furumoto, S., Tago, T., Furukawa, K., Ishiki, A., Tomita, N., Iwata, R., Tashiro, M., Arai, H., Yanai, K., et al. (2016) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-016-3453-y · Cited by 25
Xia, C., & Dickerson, B. C. (2017) · PET Clinics · doi:10.1016/j.cpet.2017.02.005 · Cited by 28
Parametric methods for [ 18 F]flortaucipir PET
Golla, S. S. V., Wolters, E. E., Timmers, T., Ossenkoppele, R., van der Weijden, C. W. J., Scheltens, P., Schwarte, L. A., Mintun, M. A., Devous, M. D., Schuit, R. C., et al. (2018) · Journal of Cerebral Blood Flow & Metabolism · doi:10.1177/0271678x18820765 · Cited by 25
Wooten, D., Ortiz-Terán, L., Zubcevik, N., Zhang, X., Huang, C., Sepulcre, J., Atassi, N., Johnson, K. A., ZAFONTE, R. D., & Fakhri, G. E. (2019) · Journal of Neurotrauma · doi:10.1089/neu.2018.6178 · Cited by 26
“In particular, [(18)F]AV-1451 has demonstrated high affinity and selectivity for tau over amyloid.(4,5) It should be noted that upon initiation of this study, [(18)F]AV-1451 was the best tau radiotracer”
BackgroundQuinuclidine and DABCO Enhance the Radiofluorination of 5‐Substituted 2‐Halopyridines
Naumiec, G. R., Cai, L., Lu, S., et al. (2017) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201700970 · Cited by 24
Tau PET Imaging for Staging of Alzheimer's Disease in Down Syndrome
Rafii, M. S. (2018) · Developmental Neurobiology · doi:10.1002/dneu.22658 · Cited by 23
“Recent PET studies have detected such tau pathology in similar brain areas in mild AD cases (Chien et al., 2013; Xia et al., 2013; Villemagne et al., 2014).”
BackgroundTauIQ: A Canonical Image Based Algorithm to Quantify Tau PET Scans
Whittington, A., Gunn, R. N., & Initiative, A. D. N. (2021) · Journal of Nuclear Medicine · doi:10.2967/jnumed.120.258962 · Cited by 24
“The development of tau imaging agents faced increased challenges due to lower target density, selectivity issues over off-target species, and the existence of different isomeric forms of tau (3R,4R) and gained traction in the following decade only with the introduction of (18)F-flortaucipir in 2013 (5).”
Imaging Biomarkers of Alzheimer Disease in Multiple Sclerosis
Zeydan, B., Lowe, V. J., Reichard, R. R., Przybelski, S. A., Lesnick, T. G., Schwarz, C. G., Senjem, M. L., Gunter, J. L., Parisi, J. E., Machulda, M. M., et al. (2020) · Annals of Neurology · doi:10.1002/ana.25684 · Cited by 27
“Pittsburgh compound B (PiB) positron emission tomography (PET) is a biomarker of β-amyloid load in plaques,1 and AV1451 tau PET is a biomarker of post-translationally modified tau protein accumulation associated with AD.2,3 Although β-amyloid and tau PET imaging are widely studied in cognitive aging and AD, little is…”
BackgroundLi, C., Fan, S., Chen, T., Chiu, M., Yen, R., & Lin, C. (2020) · Brain and Behavior · doi:10.1002/brb3.1548 · Cited by 25
“More recently, merging tau PET has shown value in diagnosis of AD and other tauopathy disorders (Chien et al., 2013; Shoup et al., 2013).”
BackgroundInfluentialSchmidt, M. E., Janssens, L., Moechars, D., Rombouts, F. J. R., Timmers, M., Barret, O., Constantinescu, C. C., Madonia, J., Russell, D., Sandiego, C. M., et al. (2020) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-020-04880-1 · Cited by 22
Self-citationInteractions between Microtubule-Associated Protein Tau (MAPT) and Small MoleculesPreprint
Rauch, J. N., Olson, S. H., & Gestwicki, J. E. (2016) · Cold Spring Harbor Perspectives in Medicine · doi:10.1101/cshperspect.a024034 · Cited by 22
Sigurdsson, E. M. (2013) · Neurodegenerative Diseases · doi:10.1159/000354491 · Cited by 23
“In vivo imaging of Aβ plaques using compounds that bind well to β-sheets is already in clinical use but only a few tau-binding ligands have been identified in preclinical studies [20–23], and some of those have failed in clinical trials [24], while others are still being evaluated [23].”
Selective Tau Imaging: Der Stand der Dinge
Villemagne, V. L. (2017) · Journal of Nuclear Medicine · doi:10.2967/jnumed.117.198325 · Cited by 24
“Besides 18F-AV1415 (3,8), among the first generation of selective tau tracers for PET is 11C-PBB3 (4), and the series developed by Tohoku (THK) University in Sendai, Japan, namely 18F-THK5317 (17) and 18F-THK5351 (Fig.”
Background18F-THK5351 Positron Emission Tomography Imaging in Neurodegenerative Tauopathies
Ezura, M., Kikuchi, A., Okamura, N., Ishiki, A., Hasegawa, T., Harada, R., Watanuki, S., Funaki, Y., Hiraoka, K., Baba, T., et al. (2021) · Frontiers in Aging Neuroscience · doi:10.3389/fnagi.2021.761010 · Cited by 25
“Tau PET studies have been performed in patients with CBS, PSP, and AD (Dani et al., 2016; Coakeley and Strafella, 2017).”
BackgroundNeuronal PET tracers for Alzheimer's disease.
Kumar, A. P., Singh, N., Nair, D. R., & Justin, A. (2021) · Biochemical and Biophysical Research Communications - BBRC · doi:10.1016/j.bbrc.2021.11.093 · Cited by 15
Künze, G., Kümpfel, R., Rullmann, M., Barthel, H., Brendel, M., Patt, M., & Sabri, O. (2022) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.2c00291 · Cited by 22
Investigating Tau and Amyloid Tracer Skull Binding in Studies of Alzheimer Disease
Flores, S. E., Chen, C. D., Su, Y., Dincer, A., Keefe, S., McKay, N. S., Paulick, A. M., Guzmán, G., Wang, L. Y., Hornbeck, R. C., et al. (2022) · Journal of Nuclear Medicine · doi:10.2967/jnumed.122.263948 · Cited by 22
Insight into the Molecular Imaging of Alzheimer’s Disease
Arora, A., & Bhagat, N. (2016) · International Journal of Biomedical Imaging · doi:10.1155/2016/7462014 · Cited by 23
“(18)F-T807 PET based studies in AD patients have shown cortical localization of the radiotracer that is consistent with the known distribution of PHF tau in the brain [139].”
ResultPrevention Trials in Alzheimer’s Disease: Current Status and Future Perspectives
Wang, J., Tan, L., & Yu, J. (2016) · Journal of Alzheimer s Disease · doi:10.3233/jad-150826 · Cited by 24
Biodistribution and Radiation Dosimetry for the Tau Tracer 18F-THK-5351 in Healthy Human Subjects
Hsiao, I., Lin, K., Huang, K., Huang, C., Chen, H.-S., Wey, S., Yen, T., Okamura, N., & Hsu, J. (2017) · Journal of Nuclear Medicine · doi:10.2967/jnumed.116.189126 · Cited by 23
“Some of the proposed tau tracers have met these criteria and are currently undergoing clinical assessments, including the THK analogs 18F-THK-5105, 18F-THK-5117 (16), 11C-PBB3 (17), and 18F-AV-1451 (formerly called 18F-T807) (19).”
BackgroundLigands for Protein Fibrils of Amyloid-β, α-Synuclein, and Tau
Chisholm, T. S., & Hunter, C. A. (2025) · Chemical Reviews · doi:10.1021/acs.chemrev.4c00838 · Cited by 26
Novel PET/SPECT Probes for Imaging of Tau in Alzheimer’s Disease
Watanabe, H., Ono, M., & Saji, H. (2015) · The Scientific World JOURNAL · doi:10.1155/2015/124192 · Cited by 22
“These preliminary results suggested that [(18)F]T807 and [(18)F]T808 have promise for the in vivo imaging of tau in AD patients [34, 35].”
ResultAdvances in PET Imaging of Degenerative, Cerebrovascular, and Traumatic Causes of Dementia
Eisenmenger, L. B., Huo, E. J., Hoffman, J. M., Minoshima, S., Matesan, M. C., Lewis, D. H., Lopresti, B. J., Mathis, C. A., Okonkwo, D. O., & Mountz, J. M. (2015) · Seminars in Nuclear Medicine · doi:10.1053/j.semnuclmed.2015.09.003 · Cited by 21
Molecular Imaging of Fluorinated Probes for Tau Protein and Amyloid-β Detection
Yeo, S. K., Shepelytskyi, Y., Grynko, V., & Albert, M. S. (2020) · Molecules · doi:10.3390/molecules25153413 · Cited by 22
“Human 18F-T807 PET studies show high-target cortical-to-cerebellum ratios and accumulations in brain regions associated with the distribution of PHF-tau in AD brains [66].”
BackgroundKara, F., Joers, J. M., Deelchand, D. K., Park, Y. W., Przybelski, S. A., Lesnick, T. G., Senjem, M. L., Zeydan, B., Knopman, D. S., Lowe, V. J., et al. (2022) · Neurobiology of Aging · doi:10.1016/j.neurobiolaging.2021.12.010 · Cited by 22
The clinical importance of suspected non-Alzheimer disease pathophysiology
Vos, S. J. B., Delvenne, A., Jack, C. R., Thal, D. R., & Visser, P. J. (2024) · Nature Reviews Neurology · doi:10.1038/s41582-024-00962-y · Cited by 23
“To enable these recommendations to be applied in research environments where either imaging or CSF biomarkers were used, CSF tau (for which a measure did exist) was grouped together with MRI and 18 F-FDG PET into a tau-related neurodegeneration or ‘N’ group 3 — a practical but imperfect solution.”
Influential
Metadata
- Authors
- Chien, D. T., Bahri, S., Szardenings, A. K., Walsh, J. C., Mu, F., Su, M.-Y., Shankle, W. R., Elizarov, A., & Kolb, H. C.
- Affiliations
- Siemens Molecular Imaging, Inc., Culver City, CA, USA
- University of California, Irvine (US)
- Hoag Memorial Hospital Presbyterian (US)
- Venue
- Journal of Alzheimer's Disease
- Publisher
- SAGE Publications
- Published
- 2013-06-20
- Volume
- 34
- Issue
- 2
- Pages
- 457-468
- ISSN
- 1387-2877 (ISSN-L)
- 1875-8908
- OpenAlex
- W4235092975
- Cited by
- 651
- References
- 0
- Citations by year
- 2026: 14 · 2025: 26 · 2024: 19 · 2023: 31 · 2022: 40 · 2021: 51 · 2020: 49 · 2019: 49 · 2018: 57 · 2017: 88 · 2016: 87 · 2015: 62 · 2014: 54 · 2013: 23
- FWCI
- 52.32
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Alzheimer s Disease (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Alzheimer's disease research and treatments
- Health Sciences › Medicine › Psychiatry and Mental health › Dementia and Cognitive Impairment Research
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Medical Imaging Techniques and Applications
- Keywords
- PHF-tau
- MeSH terms
- Aged, Aged, 80 and over, Alzheimer Disease, Carbolines, Female, Fluorine Radioisotopes, Frontal Lobe, Humans, Male, Middle Aged, Phosphorylation, tau Proteins, Early Diagnosis, Positron-Emission Tomography
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