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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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NIA‐AA Research Framework: Toward a biological definition of Alzheimer's disease
Jack, C. R., Bennett, D. A., Blennow, K., Carrillo, M. C., Dunn, B., Haeberlein, S. B., Holtzman, D. M., Jagust, W., Jessen, F., Karlawish, J., et al. (2018) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2018.02.018 · Cited by 10,537
“However, at least one firstgeneration ligand has emerged as a reliable biomarker of 3R/4R PHF tau deposits [28].”
The amyloid hypothesis of Alzheimer's disease at 25 years
Selkoe, D. J., & Hardy, J. (2016) · EMBO Molecular Medicine · doi:10.15252/emmm.201606210 · Cited by 6,164
“The recent development of imaging agents for tangles (Chien et al, 2013; Liang et al, 2014) will help define the time course of accrual of the two major lesions, although tangles are somewhat non-specific in that they occur increasingly with “normal” aging and in several neurodegenerative processes…”
BackgroundPROTAC targeted protein degraders: the past is prologue
Békés, M., Langley, D. R., & Crews, C. M. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00371-6 · Cited by 3,395
2018 Alzheimer's disease facts and figures
Alzheimer's Association (2018) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2018.02.001 · Cited by 1,912
Preclinical Alzheimer’s Disease: Definition, Natural History, and Diagnostic Criteria
Dubois, B., Hampel, H., Feldman, H. H., Scheltens, P., Aisen, P., Andrieu, S., Bakardjian, H., Benali, H., Bertram, L., Blennow, K., et al. (2016) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2016.02.002 · Cited by 1,925
“Early human studies show (even with small numbers) the expected correlations with cognitive state and brain atrophy [83,85,86].”
BackgroundThe Centiloid Project: standardizing quantitative amyloid plaque estimation by PET
Klunk, W. E., Koeppe, R. A., Price, J. C., Benzinger, T. L., Devous, M. D., Jagust, W. J., Johnson, K. A., Mathis, C. A., Minhas, D., Pontecorvo, M. J., et al. (2015) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2014.07.003 · Cited by 1,348
“It should be noted that while this process was developed with amyloid imaging data in mind, an analogous approach could be used for most any class of tracers, including emerging tau tracers [28-30].”
MethodPET Imaging of Tau Deposition in the Aging Human Brain
Schöll, M., Lockhart, S. N., Schonhaut, D. R., O’Neil, J. P., Janabi, M., Ossenkoppele, R., Baker, S. L., Vogel, J. W., Faria, J., Schwimmer, H. D., et al. (2016) · Neuron · doi:10.1016/j.neuron.2016.01.028 · Cited by 1,214
“Human studies indicate binding patterns that parallel existing neuropathological staging of tau and which increase in the presence of cognitive impairment and dementia (Chien et al., 2013; Johnson et al., 2015).”
Tau PET patterns mirror clinical and neuroanatomical variability in Alzheimer’s disease
Ossenkoppele, R., Schonhaut, D. R., Schöll, M., Lockhart, S. N., Ayakta, N., Baker, S. L., O’Neil, J. P., Janabi, M., Lazaris, A., Cantwell, A., et al. (2016) · Brain · doi:10.1093/brain/aww027 · Cited by 1,185
“The recent advent of a PET tracer (i.e. 18F-AV1451, formerly called 18F-T807), which shows high affinity and selectivity for paired helical filament tau pathology in vitro (Chien et al., 2013; Xia et al., 2013; Marquie et al., 2015), now allows in vivo assessment of regional tau load.”
BackgroundMethodInfluentialTau pathology and neurodegeneration
Spillantini, M. G., & Goedert, M. (2013) · The Lancet Neurology · doi:10.1016/s1474-4422(13)70090-5 · Cited by 1,133
Biomarker Modeling of Alzheimer’s Disease
Jack, C. R., & Holtzman, D. M. (2013) · Neuron · doi:10.1016/j.neuron.2013.12.003 · Cited by 1,002
Tau positron emission tomographic imaging in aging and early Alzheimer disease
Johnson, K. A., Schultz, A., Betensky, R. A., Becker, J. A., Sepulcre, J., Rentz, D., Mormino, E., Chhatwal, J., Amariglio, R., Papp, K., et al. (2016) · Annals of Neurology · doi:10.1002/ana.24546 · Cited by 986
“smoothed with an 8mm Gaussian kernel to account for individual anatomic differences.(7) (11)C PiB PET data were expressed as the distribution volume ratio (DVR) with cerebellar gray as reference tissue; regional time–activity curves were used to compute regional DVRs for each ROI using the Logan graphical method appli…”
MethodResultInfluentialTau and neurodegenerative disease: the story so far
Iqbal, K., Liu, F., & Gong, C.-X. (2016) · Nature Reviews Neurology · doi:10.1038/nrneurol.2015.225 · Cited by 806
The neuropathology of traumatic brain injury
McKee, A. C., & Daneshvar, D. H. (2015) · Handbook of clinical neurology · doi:10.1016/b978-0-444-52892-6.00004-0 · Cited by 899
Spreading of pathology in neurodegenerative diseases: a focus on human studies
Brettschneider, J., Tredici, K. D., Lee, V. M.-Y., & Trojanowski, J. Q. (2015) · Nature Reviews Neuroscience · doi:10.1038/nrn3887 · Cited by 790
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Tau and Aβ imaging, CSF measures, and cognition in Alzheimer’s disease
Brier, M. R., Gordon, B., Friedrichsen, K., McCarthy, J., Stern, A., Christensen, J., Owen, C., Aldea, P., Su, Y., Hassenstab, J., et al. (2016) · Science Translational Medicine · doi:10.1126/scitranslmed.aaf2362 · Cited by 734
“Each participant underwent T807 (tau) (20) and florbetapir (Aβ) positron emission”
The Evolution of Preclinical Alzheimer’s Disease: Implications for Prevention Trials
Sperling, R., Mormino, E., & Johnson, K. (2014) · Neuron · doi:10.1016/j.neuron.2014.10.038 · Cited by 725
Early Clinical PET Imaging Results with the Novel PHF-Tau Radioligand [F18]-T808
Chien, D. T., Szardenings, A. K., Bahri, S., Walsh, J. C., Mu, F., Xia, C. A., Shankle, W. R., Lerner, A. J., Su, M., Elizarov, A. M., et al. (2013) · Journal of Alzheimer s Disease · doi:10.3233/jad-130098 · Cited by 683
“reported initial clinical results of a first-in-man study with the novel PHF-tau PET radiotracer [F18]-T807 [8].”
Self-citationArendt, T., Stieler, J. T., & Holzer, M. (2016) · Brain Research Bulletin · doi:10.1016/j.brainresbull.2016.08.018 · Cited by 609
Marquié, M., Normandin, M. D., Vanderburg, C. R., Costantino, I. M., Bien, E. A., Rycyna, L. G., Klunk, W. E., Mathis, C. A., Ikonomovic, M. D., Debnath, M. L., et al. (2015) · Annals of Neurology · doi:10.1002/ana.24517 · Cited by 615
“The first emerging data from in vivo human [F-18]-AV-1451 PET scans pointed to a significantly higher [F-18]-AV-1451 retention in the brain of patients with AD when compared to individuals with MCI and cognitively normal control subjects.(3) In agreement with these observations, our recent in vivo studies based on [F-…”
BackgroundResultTau PET imaging in neurodegenerative tauopathies—still a challenge
Leuzy, A., Chiotis, K., Lemoine, L., Gillberg, P.-G., Almkvist, O., Rodriguez-Vieitez, E., & Nordberg, A. (2019) · Molecular Psychiatry · doi:10.1038/s41380-018-0342-8 · Cited by 628
Arboleda-Velasquez, J. F., Lopera, F., O’Hare, M., Delgado-Tirado, S., Marino, C., Chmielewska, N., Saez-Torres, K. L., Amarnani, D., Schultz, A. P., Sperling, R. A., et al. (2019) · Nature Medicine · doi:10.1038/s41591-019-0611-3 · Cited by 598
La Joie, R., Visani, A. V., Baker, S. L., Brown, J. A., Bourakova, V., Cha, J., Chaudhary, K., Edwards, L., Iaccarino, L., Janabi, M., et al. (2020) · Science Translational Medicine · doi:10.1126/scitranslmed.aau5732 · Cited by 612
The Neuropathology of Chronic Traumatic Encephalopathy
McKee, A. C., Stein, T. D., Kiernan, P. T., & Alvarez, V. E. (2015) · Brain Pathology · doi:10.1111/bpa.12248 · Cited by 585
“P-tau-specific PET ligands, such as T-807 and T-808 reported by Chien et al (13) might prove to identify primary tauopathy, such as CTE, and p-tau PET imaging combined with PET imaging for Aß might be useful to differentiate between CTE and AD (3, 44, 67).”
BackgroundDeVos, S. L., Miller, R. L., Schoch, K. M., Holmes, B. B., Kebodeaux, C. S., Wegener, A. J., Chen, G., Shen, T., Tran, H., Nichols, B., et al. (2017) · Science Translational Medicine · doi:10.1126/scitranslmed.aag0481 · Cited by 516
“Although still in the early characterization stages, we anticipate that tau positron emission tomography (PET) ligands will, in the near future, help distinguish FTD with tau from other FTD cases and thus enable a tau-focused therapeutic trial in the FTD patient population (44).”
BackgroundTau imaging: early progress and future directions
Villemagne, V. L., Fodero-Tavoletti, M. T., Masters, C. L., & Rowe, C. C. (2015) · The Lancet Neurology · doi:10.1016/s1474-4422(14)70252-2 · Cited by 501
An autoradiographic evaluation of AV-1451 Tau PET in dementia
Lowe, V. J., Curran, G., Fang, P., Liesinger, A. M., Josephs, K. A., Parisi, J. E., Kantarci, K., Boeve, B. F., Pandey, M. K., Bruinsma, T., et al. (2016) · Acta Neuropathologica Communications · doi:10.1186/s40478-016-0315-6 · Cited by 474
“PET imaging with AV1451 has shown highly specific binding affinity to tau in AD patients [17, 18].”
BackgroundComparison of multiple tau-PET measures as biomarkers in aging and Alzheimer's disease
Maass, A., Landau, S., Baker, S. L., Horng, A., Lockhart, S. N., La Joie, R., Rabinovici, G. D., & Jagust, W. J. (2017) · NeuroImage · doi:10.1016/j.neuroimage.2017.05.058 · Cited by 462
“MARK filament tau in AD patients (Chien et al., 2013; Lowe et al., 2016; Marquié et al., 2015).”
BackgroundFleisher, A. S., Pontecorvo, M. J., Devous, M. D., Lu, M., Arora, A. K., Truocchio, S. P., Aldea, P., Flitter, M., Locascio, T., Devine, M., et al. (2020) · JAMA Neurology · doi:10.1001/jamaneurol.2020.0528 · Cited by 448
Imaging tau and amyloid-β proteinopathies in Alzheimer disease and other conditions
Villemagne, V. L., Doré, V., Burnham, S. C., Masters, C. L., & Rowe, C. C. (2018) · Nature Reviews Neurology · doi:10.1038/nrneurol.2018.9 · Cited by 447
Ghetti, B. F., Oblak, A. L., Boeve, B. F., Johnson, K. A., Dickerson, B. C., & Goedert, M. (2014) · Neuropathology and Applied Neurobiology · doi:10.1111/nan.12213 · Cited by 458
Schwarz, A. J., Yu, P., Miller, B. B., Shcherbinin, S., Dickson, J., Navitsky, M., Joshi, A. D., Devous, M. D., & Mintun, M. S. (2016) · Brain · doi:10.1093/brain/aww023 · Cited by 425
“, 2015), and to exhibit favourable kinetics, low non-specific binding and differential uptake in Alzheimer’s disease versus healthy control subjects (Chien et al., 2013).”
BackgroundMcKee, A. C., Daneshvar, D. H., Alvarez, V. E., & Stein, T. D. (2014) · Acta Neuropathologica · doi:10.1007/s00401-013-1230-6 · Cited by 422
“…the development of CTE will be greatly facilitated by efforts to develop a highly specific and sensitive way to diagnose CTE in living persons, such as with new PET tau ligands [29, 119, 198, 201], as well as prospective longitudinal studies with accurate measures of cumulative traumatic exposures.”
BackgroundSuárez‐Calvet, M., Karikari, T. K., Ashton, N. J., Lantero Rodríguez, J., Milà‐Alomà, M., Gispert, J. D., Salvadó, G., Minguillon, C., Fauria, K., Shekari, M., et al. (2020) · EMBO Molecular Medicine · doi:10.15252/emmm.202012921 · Cited by 401
“Furthermore, in a pathological study discriminating insoluble NFT from soluble oligomeric and detergent-soluble tau, phosphorylation at threonine-231 was one of the consistently increased tau posttranslational modifications that discriminated Braak stage 0–”
ResultInfluentialMild Cognitive Impairment and Mild Dementia: A Clinical Perspective
Knopman, D. S., & Petersen, R. C. (2014) · Mayo Clinic Proceedings · doi:10.1016/j.mayocp.2014.06.019 · Cited by 423
“Positron emission tomography for detection of tau protein is also being studied in the research setting.(40) A combination of imaging or cerebrospinal fluid studies has been introduced for research purposes into the diagnostic criteria forMCI (and dementia).”
MethodRadiopharmaceuticals for PET and SPECT Imaging: A Literature Review over the Last Decade
Crișan, G., Moldovean‐Cioroianu, N. S., Timaru, D.-G., Andrieș, G., Cainap, C. I., & Chiş, V. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23095023 · Cited by 386
18F-THK5351: A Novel PET Radiotracer for Imaging Neurofibrillary Pathology in Alzheimer Disease
Harada, R., Okamura, N., Furumoto, S., Furukawa, K., Ishiki, A., Tomita, N., Tago, T., Hiraoka, K., Watanuki, S., Shidahara, M., et al. (2016) · Journal of Nuclear Medicine · doi:10.2967/jnumed.115.164848 · Cited by 330
Schultz, A. P., Chhatwal, J. P., Hedden, T., Mormino, E. C., Hanseeuw, B. J., Sepulcre, J., Huijbers, W., LaPoint, M., Buckley, R. F., Johnson, K. A., et al. (2017) · The Journal of Neuroscience · doi:10.1523/jneurosci.3263-16.2017 · Cited by 330
“For both PiB and AV1451, we used a cerebellar gray matter reference region from the Freesurfer aseg atlas, as previously described (Becker et al., 2011; Chien et al., 2013; Johnson et al., 2016), with AV1451 measures computed as standardized uptake value ratios (SUVRs) from the 80 –100 min time frame and PiB measures…”
MethodMoloney, C. M., Lowe, V. J., & Murray, M. E. (2021) · Alzheimer s & Dementia · doi:10.1002/alz.12321 · Cited by 358
Developing the ATX(N) classification for use across the Alzheimer disease continuum
Hampel, H. J., Cummings, J. L., Blennow, K., Gao, P., Jack, C. R., & Vergallo, A. (2021) · Nature Reviews Neurology · doi:10.1038/s41582-021-00520-w · Cited by 351
Jack, C. R., Wiste, H. J., Therneau, T. M., Weigand, S. D., Knopman, D. S., Mielke, M. M., Lowe, V. J., Vemuri, P., Machulda, M. M., Schwarz, C. G., et al. (2019) · JAMA · doi:10.1001/jama.2019.7437 · Cited by 324
“A−T−(N)− A−T+(N)− A−T−(N)+ A−T+(N)+ A+T−(N)− A+T+(N)− A+T−(N)+ A+T+(N)+ Participants 140 (29) 33 (7) 81 (17) 22 (5) 54 (11) 24 (5) 69 (14) 57 (12)”
Jack, C. R., Therneau, T. M., Weigand, S. D., Wiste, H. J., Knopman, D. S., Vemuri, P., Lowe, V. J., Mielke, M. M., Roberts, R. O., Machulda, M. M., et al. (2019) · JAMA Neurology · doi:10.1001/jamaneurol.2019.1971 · Cited by 300
Lewczuk, P., Riederer, P. F., O’Bryant, S. E., Verbeek, M. M., Dubois, B., Visser, P. J., Jellinger, K. A., Engelborghs, S., Ramírez, A., Parnetti, L., et al. (2017) · The World Journal of Biological Psychiatry · doi:10.1080/15622975.2017.1375556 · Cited by 318
“…has demonstrated increased tracer binding in lateral temporal regions in pre-clinical individuals and further uptake in the temporal lobe, lateral occipital cortex and temporal parietal junction in later disease stages (Chien et al. 2013; Gordon, Friedrichsen, et al. 2016; Johnson et al. 2016).”
BackgroundSuspected non-Alzheimer disease pathophysiology — concept and controversy
Jack, C. R., Knopman, D. S., Chételat, G., Dickson, D. W., Fagan, A. M., Frisoni, G. B., Jagust, W. J., Mormino, E. C., Petersen, R. C., Sperling, R. A., et al. (2016) · Nature Reviews Neurology · doi:10.1038/nrneurol.2015.251 · Cited by 313
The Alzheimer's Disease Neuroimaging Initiative 2 PET Core: 2015
Jagust, W. J., Landau, S. M., Koeppe, R. A., Reiman, E. M., Chen, K., Mathis, C. A., Price, J. C., Foster, N. L., & Wang, A. Y. (2015) · Alzheimer s & Dementia · doi:10.1016/j.jalz.2015.05.001 · Cited by 302
Wang, L. Y., Benzinger, T. L. S., Su, Y., Christensen, J. J., Friedrichsen, K. A., Aldea, P., McConathy, J., Cairns, N. J., Fagan, A. M., Morris, J. C., et al. (2016) · JAMA Neurology · doi:10.1001/jamaneurol.2016.2078 · Cited by 301
van Oostveen, W. M., & de Lange, E. C. M. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22042110 · Cited by 297
“Although 18F−T808 exhibited high tau affinity, rapid uptake and clearance, a disadvantage of this compound was de defluorination followed by bone uptake of 18F [139].”
BackgroundThe impact of amyloid‐beta and tau on prospective cognitive decline in older individuals
Sperling, R. A., Mormino, E. C., Schultz, A. P., Betensky, R. A., Papp, K. V., Amariglio, R. E., Hanseeuw, B. J., Buckley, R., Chhatwal, J., Hedden, T., et al. (2019) · Annals of Neurology · doi:10.1002/ana.25395 · Cited by 286
Tau PET imaging: present and future directions
Saint‐Aubert, L., Lemoine, L., Chiotis, K., Leuzy, A., Rodriguez‐Vieitez, E., & Nordberg, A. K. (2017) · Molecular Neurodegeneration · doi:10.1186/s13024-017-0162-3 · Cited by 300
“Other groups using [(18)F]AV-1451 in vivo substantiated these findings by reporting good discrimination between AD dementia patients and CN subjects, with greater cortical retention in patients, mostly within the temporal cortex [22, 45, 56, 59, 61].”
ResultXia, C., Makaretz, S. J., Caso, C., McGinnis, S. M., Gomperts, S. N., Sepulcre, J., Gómez‐Isla, T., Hyman, B. T., Schultz, A. P., Vasdev, N., et al. (2017) · JAMA Neurology · doi:10.1001/jamaneurol.2016.5755 · Cited by 288
“The first use of the ligand now known as [(18)F]AV-1451 in patients with AD was reported in 2013.(25) The selectivity of this ligand forhyperphosphorylated tauwas recently confirmed.”
McAleese, K. E., Walker, L., Graham, S., Moya, E. L. J., Johnson, M. A., Erskine, D., Colloby, S. J., Dey, M., Martin-Ruiz, C. M., Taylor, J., et al. (2017) · Acta Neuropathologica · doi:10.1007/s00401-017-1738-2 · Cited by 280
“As mentioned previously, our study focused on parietal WML and prior work suggests that the aetiology of WML differs by anatomical location [34], hence, further imaging studies that also involve new in vivo imaging of HPτ [11] and Aβ [32] pathology and integrate anatomical location, pathophysiology and impact on cogni…”
Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models
Silva, M. C., Ferguson, F. M., Cai, Q., Donovan, K. A., Nandi, G., Patnaik, D., Zhang, T., Huang, H.-T., Lucente, D. E., Dickerson, B. C., et al. (2019) · eLife · doi:10.7554/elife.45457 · Cited by 283
“…degraded at concentrations as low as 100 nM QC-01– 175, whereas maximal total tau clearance (Dmax, 24h) was achieved at 10 mM, consistent with expected binding preference of a T807-derivative for insoluble P-tau (Chien et al., 2013; Lowe et al., 2016; Marquié et al., 2015; Xia et al., 2013).”
BackgroundMethodResultHostetler, E. D., Walji, A. M., Zeng, Z., Miller, P. J., Bennacef, I., Salinas, C. A., Connolly, B., Gantert, L. T., Haley, H., Holahan, M. A., et al. (2016) · Journal of Nuclear Medicine · doi:10.2967/jnumed.115.171678 · Cited by 283
“18F-AV-1451 (18F-T807) was the first PET tracer to show promise for quantifying NFT pathology in AD patients (7) and is currently the most widely studied NFT PET tracer.”
BackgroundAcute and chronic traumatic encephalopathies: pathogenesis and biomarkers
DeKosky, S. T., Blennow, K., Ikonomović, M. D., & Gandy, S. (2013) · Nature Reviews Neurology · doi:10.1038/nrneurol.2013.36 · Cited by 273
Tau PET in Alzheimer disease and mild cognitive impairment
Cho, H., Choi, J. Y., Hwang, M. S., Lee, J., Kim, Y. J., Lee, H., Lyoo, C. H., Ryu, Y. H., & Lee, M. S. (2016) · Neurology · doi:10.1212/wnl.0000000000002892 · Cited by 274
“pathology(8,9) and a correlation between cortical tau binding and cognitive dysfunction.(7,10) These suggest that (18)F-AV-1451 can be a promising surrogate marker for in vivo imaging of tau pathology in AD.”
BackgroundStructural Imaging Measures of Brain Aging
Lockhart, S. N., & DeCarli, C. S. (2014) · Neuropsychology Review · doi:10.1007/s11065-014-9268-3 · Cited by 301
“The exact relevance of this finding awaits further research (Chien et al. 2013; Xia et al. 2013) but could suggest a more complicated process leading to age-related differences in hippocampal volume.”
BackgroundRadiological biomarkers for diagnosis in PSP: Where are we and where do we need to be?
Whitwell, J. L., Höglinger, G. U., Antonini, A., Bordelon, Y. M., Boxer, A. L., Colosimo, C., van Eimeren, T., Golbe, L. I., Kassubek, J., Kurz, C., et al. (2017) · Movement Disorders · doi:10.1002/mds.27038 · Cited by 263
Non-invasive assessment of Alzheimer’s disease neurofibrillary pathology using 18F-THK5105 PET
Okamura, N., Furumoto, S., Fodero‐Tavoletti, M. T., Mulligan, R. S., Harada, R., Yates, P. A., Pejoska, S., Kudo, Y., Masters, C. L., Yanai, K., et al. (2014) · Brain · doi:10.1093/brain/awu064 · Cited by 273
18F-MK-6240 PET for early and late detection of neurofibrillary tangles
Pascoal, T. A., Therriault, J., Benedet, A. L., Savard, M., Lussier, F. Z., Chamoun, M., Tissot, C., Qureshi, M. N. I., Kang, M. S., Mathotaarachchi, S. S., et al. (2020) · Brain · doi:10.1093/brain/awaa180 · Cited by 263
“, 2016) Although several studies have reported that (18)F-flortaucipir shows excellent performance for depict tau pathology in regions comprising late Braak stages (Chien et al., 2013; Gordon et al., 2016; Johnson et al., 2016; Scholl et al., 2016; Pontecorvo et al., 2017; Lowe et al., 2018), its performance for early…”
BackgroundTau burden and the functional connectome in Alzheimer’s disease and progressive supranuclear palsy
Cope, T., Rittman, T., Borchert, R. J., Jones, P. S., Vatansever, D., Allinson, K. S. J., Passamonti, L., Rodríguez, P. V., Bevan-Jones, W. R., O'Brien, J. T., et al. (2017) · Brain · doi:10.1093/brain/awx347 · Cited by 251
Tau immunotherapy for Alzheimer's disease
Pedersen, J. T., & Sigurdsson, E. M. (2015) · Trends in Molecular Medicine · doi:10.1016/j.molmed.2015.03.003 · Cited by 247
Atrophy patterns in early clinical stages across distinct phenotypes of Alzheimer's disease
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Impact of the Alzheimer's Disease Neuroimaging Initiative, 2004 to 2014
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“Various brain regions were analyzed for the uptake of [(18)F]T807 across healthy controls, mild cognitive impairment, and AD patients [104].”
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Orr, M. E., Sullivan, A. C., & Frost, B. E. (2017) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2017.03.011 · Cited by 242
“PET-based imaging of pathogenic tau in living humans using 18 [293_TD$DIFF] -AV1451 [17,18] has recently spurred a wealth of studies demonstrating a significant correlation between tau-positive PET, disease severity, and postmortem histopathological data for Alzheimer’s disease [18,19].”
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A Review of the Effectiveness of Neuroimaging Modalities for the Detection of Traumatic Brain Injury
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“to tau have been developed, and preliminary PET images in one study show increased binding in patients with clinical Alzheimer’s disease.(231) [(18)F]T807 has high specificity for the paired helical”
BackgroundTau Positron Emission Tomographic Imaging in the Lewy Body Diseases
Gomperts, S. N., Locascio, J. J., Makaretz, S. J., Schultz, A. P., Caso, C., Vasdev, N., Sperling, R. A., Growdon, J. H., Dickerson, B. C., & Johnson, K. A. (2016) · JAMA Neurology · doi:10.1001/jamaneurol.2016.3338 · Cited by 228
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Biomarkers for the Early Detection and Progression of Alzheimer's Disease
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“Flortaucipir was developed to bind to the 3R/4R form of pathological tau that characterizes Alzheimer’s disease (Chien et al., 2013; Lowe et al., 2016; Lemoine et al., 2017; Marquie et al., 2017).”
Ono, M., Sahara, N., Kumata, K., Ji, B., Ni, R., Koga, S., Dickson, D. W., Trojanowski, J. Q., Lee, V. M. ‐., Yoshida, M., et al. (2016) · Brain · doi:10.1093/brain/aww339 · Cited by 206
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“In the last decade, positron emission tomography (PET) radiotracers have become available to image in vivo aggregated Aβ (Klunk et al. , 2004) and PHF-tau protein (Xia et al. , 2013; Chien et al. , 2013).”
BackgroundTau-positron emission tomography correlates with neuropathology findings.
Lowe, V. J., Lundt, E. S., Albertson, S. M., Min, H., Fang, P., Przybelski, S. A., Senjem, M. L., Schwarz, C. G., Kantarci, K., Boeve, B., et al. (2020) · Alzheimer's & Dementia · doi:10.1016/j.jalz.2019.09.079 · Cited by 203
18F-AV-1451 positron emission tomography in Alzheimer’s disease and progressive supranuclear palsy
Passamonti, L., Rodríguez, P. V., Hong, Y. T., Allinson, K. S. J., Williamson, D., Borchert, R. J., Sami, S. A. K., Cope, T., Bevan-Jones, W. R., Jones, P. S., et al. (2016) · Brain · doi:10.1093/brain/aww340 · Cited by 210
“Radioligands have recently been developed for PET to measure in vivo binding to aggregated tau, including PBB3 (Maruyama et al., 2013), THK compounds (Okamura et al., 2014), and 18F-AV-1451 (Chien et al., 2013; Xia et al., 2013).”
BackgroundAccelerating Alzheimer’s therapeutic development: The past and future of clinical trials
Boxer, A. L., & Sperling, R. (2023) · Cell · doi:10.1016/j.cell.2023.09.023 · Cited by 197
“39 Data from both clinical neuropathologic comparisons, such as the Braak staging system, 40 as well as more recent studies using tau PET ligands, 41 show that both the amount and anatomical location of insoluble tau in the brain is strongly correlated with an individual’s type and severity of…”
Network Dysfunction in Alzheimer's Disease: Refining the Disconnection Hypothesis
Brier, M. R., Thomas, J., & Ances, B. M. (2014) · Brain Connectivity · doi:10.1089/brain.2014.0236 · Cited by 203
“While amyloid imaging has facilitated the direct comparison of amyloid topography and functional connectivity, tau-imaging agents have been unavailable until recently (Chien et al., 2013; Fodero-Tavoletti et al., 2011; Maruyama et al., 2013; Small et al., 2006).”
Recent Progress in Alzheimer’s Disease Research, Part 3: Diagnosis and Treatment
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Neurogenetic contributions to amyloid beta and tau spreading in the human cortex
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Pathological correlations of [F‐18]‐AV‐1451 imaging in non‐alzheimer tauopathies
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“The introduction of PET ligands thought to co-lo- calize with NFTs (Chien et al., 2013; Marquie et al., 2015; Lowe et al., 2016) has provided a new tool to understand the biological changes occurring in Alzheimer’s disease, and may be key to identifying the transition between cognitive normality and impairment.”
MethodInfluentialRepetitive Head Impacts and Chronic Traumatic Encephalopathy
McKee, A. C., Alosco, M. L., & Huber, B. R. (2016) · Neurosurgery Clinics of North America · doi:10.1016/j.nec.2016.05.009 · Cited by 207
In vivo quantification of neurofibrillary tangles with [18F]MK-6240
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18F‐AV‐1451 and CSF T‐tau and P‐tau as biomarkers in Alzheimer's disease
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“18F-AV-1451 (formerly called 18F-T807; Chien et al, 2013; Xia et al, 2013) detects AD-type tau aggregates (Marquié et al, 2015; Smith et al, 2016a), differentiates AD patients from controls (Brier et al, 2016; Gordon et al, 2016; Johnson et al, 2016; Schöll et al, 2016; Schwarz et al, 2016) and…”
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“The advent of PET tau tracers that preferentially bind to paired helical filaments (Chien et al., 2013; Xia et al., 2013; Villemagne and Okamura, 2014; Marquie et al., 2015) has provided a new method to track not only the levels of tauopathy, but also the crucial spatial propagation of tauopathy throughout the brain.”
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Burrell, J. R., Hodges, J. R., & Rowe, J. B. (2014) · Movement Disorders · doi:10.1002/mds.25872 · Cited by 185
The development and validation of tau PET tracers: current status and future directions
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Distinct 18F-AV-1451 tau PET retention patterns in early- and late-onset Alzheimer’s disease
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SPECT and PET imaging in Alzheimer’s disease
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AV-1451 PET imaging of tau pathology in preclinical Alzheimer disease: Defining a summary measure
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“Early reports have shown a relationship between increased tracer uptake and worsening cognitive status (Brier et al., 2016; Chien et al., 2013; Day et al., 2017; Gordon et al., 2016; Johnson et al., 2015; Schöll et al., 2016; Wang et al., 2016)”
BackgroundSoleimani‐Meigooni, D. N., Iaccarino, L., Joie, R. L., Baker, S. L., Bourakova, V., Boxer, A. L., Edwards, L., Eser, R. A., Gorno‐Tempini, M., Jagust, W. J., et al. (2020) · Brain · doi:10.1093/brain/awaa276 · Cited by 186
Validation of the new consensus criteria for the diagnosis of corticobasal degeneration
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In vivo evaluation of a novel tau imaging tracer for Alzheimer’s disease
Villemagne, V. L., Furumoto, S., Fodero‐Tavoletti, M. T., Mulligan, R. S., Hodges, J. R., Harada, R., Yates, P. A., Piguet, O., Pejoska, S., Doré, V., et al. (2014) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-013-2681-7 · Cited by 173
“Better tau tracers, some of them already being evaluated in humans, [23, 2527] will be required for applications such as monitoring disease progression and assess efficacy of anti-tau therapy.”
Background18 F-AV-1451 tau PET imaging correlates strongly with tau neuropathology in MAPT mutation carriers
Smith, R., Puschmann, A., Schöll, M., Ohlsson, T., van Swieten, J., Honer, M., Englund, E., & Hansson, O. (2016) · Brain · doi:10.1093/brain/aww163 · Cited by 168
“Studies using the most common PET tracer for tau pathology to date, 18F-AV-1451, demonstrated increased uptake in temporo-parietal regions in patients with Alzheimer’s disease (Chien et al., 2013; Johnson et al., 2016; Ossenkoppele et al., 2016; Smith et al., 2016).”
Method
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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