Characterization of the radiolabeled metabolite of tau PET tracer 18F-THK5351

European Journal of Nuclear Medicine and Molecular Imaging

Volumn 43, Issue 12, 2016, Pages 2211-2218

  Harada, Ryuichi ^a   Furumoto, Shozo ^a   Tago, Tetsuro ^a   Katsutoshi, Furukawa ^a   Ishiki, Aiko ^a   Tomita, Naoki ^a   Iwata, Ren ^a   Tashiro, Manabu ^a   Arai, Hiroyuki ^a   Yanai, Kazuhiko ^a,b   Kudo, Yukitsuka ^a   Okamura, Nobuyuki ^a,c  

^a TOHOKU UNIVERSITY   (Japan)

^b TOHOKU UNIVERSITY SCHOOL OF MEDICINE   (Japan)

^c TOHOKU PHARMACEUTICAL UNIVERSITY   (Japan)

Author keywords

Alzheimer s disease; PET; Radiolabeled metabolite; Tau

Indexed keywords

6 [(3 FLUORO 2 HYDROXY)PROPOXY] 2 (2 METHYLAMINOPYRID 5 YL)QUINOLINE F 18; DRUG METABOLITE; TAU PROTEIN; TRACER; UNCLASSIFIED DRUG; AMINOPYRIDINE DERIVATIVE; MAPT PROTEIN, HUMAN; QUINOLINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT; THK5351;

ADULT; AGED; ALZHEIMER DISEASE; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD BRAIN BARRIER; BLOOD SAMPLING; CONTROLLED STUDY; DRUG IDENTIFICATION; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; HUMAN; HUMAN TISSUE; ISOTOPE LABELING; MALE; MIDDLE AGED; MOUSE; NONHUMAN; PERMEABILITY BARRIER; POSITRON EMISSION TOMOGRAPHY; ANIMAL; BLOOD; DIAGNOSTIC IMAGING; INSTITUTE FOR CANCER RESEARCH MOUSE; METABOLIC CLEARANCE RATE; METABOLISM; MOLECULAR IMAGING; PROCEDURES; SYNTHESIS; TISSUE DISTRIBUTION;

AGED; AMINOPYRIDINES; ANIMALS; BLOOD-BRAIN BARRIER; FEMALE; HUMANS; ISOTOPE LABELING; MALE; METABOLIC CLEARANCE RATE; MICE; MICE, INBRED ICR; MOLECULAR IMAGING; QUINOLINES; RADIOPHARMACEUTICALS; TAU PROTEINS; TISSUE DISTRIBUTION;

EID: 84978758991     PISSN: 16197070     EISSN: 16197089     Source Type: Journal    
DOI: 10.1007/s00259-016-3453-y     Document Type: Article

References (32)

1. Guillozet AL, Weintraub S, Mash DC, Mesulam MM. Neurofibrillary tangles, amyloid, and memory in aging and mild cognitive impairment. Arch Neurol. 2003;60:729–36. doi:10.1001/archneur.60.5.729.
2. Giacobini E, Gold G. Alzheimer disease therapy-moving from amyloid-β to tau. Nat Rev Neurol. 2013;9:677–86. doi:10.1038/nrneurol.2013.223.
3. Braak H, Braak E. Neuropathological stageing of Alzheimer-related changes. Acta Neuropathol. 1991;82:239–59.
4. Delacourte A, David JP, Sergeant N, Buee L, Wattez A, Vermersch P, et al. The biochemical pathway of neurofibrillary degeneration in aging and Alzheimer’s disease. Neurology. 1999;52:1158–65.
5. Braak H, Alafuzoff I, Arzberger T, Kretzschmar H, Del Tredici K. Staging of Alzheimer disease-associated neurofibrillary pathology using paraffin sections and immunocytochemistry. Acta Neuropathol. 2006;112:389–404. doi:10.1007/s00401-006-0127-z.
6. Villemagne VL, Furumoto S, Fodero-Tavoletti MT, Harada R, Mulligan RS, Kudo Y, et al. The challenges of Tau imaging. Future Neurol. 2012;7:409–21.
7. Okamura N, Harada R, Furumoto S, Arai H, Yanai K, Kudo Y. Tau PET imaging in Alzheimer’s disease. Curr Neurol Neurosci Rep. 2014;14:500. doi:10.1007/s11910-014-0500-6.
8. Maruyama M, Shimada H, Suhara T, Shinotoh H, Ji B, Maeda J, et al. Imaging of tau pathology in a tauopathy mouse model and in Alzheimer patients compared to normal controls. Neuron. 2013;79:1094–108. doi:10.1016/j.neuron.2013.07.037.
9. Chien DT, Bahri S, Szardenings AK, Walsh JC, Mu F, Su MY, et al. Early clinical PET imaging results with the novel PHF-tau radioligand [F-18]-T807. J Alzheimers Dis. 2013;34:457–68. doi:10.3233/JAD-122059.
10. Chien DT, Szardenings AK, Bahri S, Walsh JC, Mu F, Xia C, et al. Early clinical PET imaging results with the novel PHF-tau radioligand [F18]-T808. J Alzheimers Dis. 2014;38:171–84. doi:10.3233/JAD-130098.
11. Harada R, Okamura N, Furumoto S, Furukawa K, Ishiki A, Tomita N, et al. 18F-THK5351: a novel PET radiotracer for imaging neurofibrillary pathology in Alzheimer disease. J Nucl Med. 2016;57:208–14. doi:10.2967/jnumed.115.164848.
12. Pike VW. PET radiotracers: crossing the blood–brain barrier and surviving metabolism. Trends Pharmacol Sci. 2009;30:431–40. doi:10.1016/j.tips.2009.05.005.
13. Tago T, Furumoto S, Okamura N, Harada R, Adachi H, Ishikawa Y, et al. Structure-activity relationship of 2-arylquinolines as PET imaging tracers for Tau pathology in Alzheimer’s disease. J Nucl Med. 2016;57:608–14. doi:10.2967/jnumed.115.166652.
14. Cole GB, Keum G, Liu J, Small GW, Satyamurthy N, Kepe V, et al. Specific estrogen sulfotransferase (SULT1E1) substrates and molecular imaging probe candidates. Proc Natl Acad Sci U S A. 2010;107:6222–7. doi:10.1073/pnas.0914904107.
15. 18F]THK-5117 PET for assessing neurofibrillary pathology in Alzheimer’s disease. Eur J Nucl Med Mol Imaging. 2015;42:1052–61. doi:10.1007/s00259-015-3035-4.
16. Okamura N, Furumoto S, Harada R, Tago T, Yoshikawa T, Fodero-Tavoletti M, et al. Novel 18F-labeled arylquinoline derivatives for noninvasive imaging of tau pathology in Alzheimer disease. J Nucl Med. 2013;54:1420–7. doi:10.2967/jnumed.112.117341.
17. Sepe V, Ummarino R, D’Auria MV, Renga B, Fiorucci S, Zampella A. The first total synthesis of solomonsterol B, a marine pregnane X receptor agonist. Eur J Org Chem. 2012;2012:5187–94. doi:10.1002/ejoc.201200619.
18. Gamage N, Barnett A, Hempel N, Duggleby RG, Windmill KF, Martin JL, et al. Human sulfotransferases and their role in chemical metabolism. Toxicol Sci. 2006;90:5–22. doi:10.1093/toxsci/kfj061.
19. Villemagne VL, Fodero-Tavoletti MT, Masters CL, Rowe CC. Tau imaging: early progress and future directions. Lancet Neurol. 2015;14:114–24.
20. Zhang W, Arteaga J, Cashion DK, Chen G, Gangadharmath U, Gomez LF, et al. A highly selective and specific PET tracer for imaging of tau pathologies. J Alzheimers Dis. 2012;31:601–12. doi:10.3233/JAD-2012-120712.
21. 18F]FDDNP and cerebral uptake of its labelled metabolites. Nucl Med Biol. 2008;35:869–74. doi:10.1016/j.nucmedbio.2008.09.002.
22. 11C-PBB3 as a clinically useful PET probe for imaging of tau pathology. J Nucl Med. 2014;55:1532–8. doi:10.2967/jnumed.114.139550.
23. Yaqub M, Boellaard R, van Berckel BN, Tolboom N, Luurtsema G, Dijkstra AA, et al. Evaluation of tracer kinetic models for analysis of [18F]FDDNP studies. Mol Imaging Biol. 2009;11:322–33. doi:10.1007/s11307-009-0208-1.
24. Kimura Y, Ichise M, Ito H, Shimada H, Ikoma Y, Seki C, et al. PET quantification of Tau pathology in human brain with 11C-PBB3. J Nucl Med. 2015;56:1359–65. doi:10.2967/jnumed.115.160127.
25. Xia CF, Arteaga J, Chen G, Gangadharmath U, Gomez LF, Kasi D, et al. [(18)F]T807, a novel tau positron emission tomography imaging agent for Alzheimer’s disease. Alzheimers Dement. 2013;9:666–76. doi:10.1016/j.jalz.2012.11.008.
26. Normandin M, Collier T, Wooten D, Kolnick A, Yokell D, Shoup T, et al. Pharmacokinetic evaluation of the tau radiotracer [F-18]T807 and cerebral binding in a subject with traumatic brain injury. J Nucl Med. 2014;55.
27. 18F-THK5117 as a PET tracer for assessing tau pathology. J Nucl Med. 2016. doi:10.2967/jnumed.115.158519.
28. Price JC, Klunk WE, Lopresti BJ, Lu X, Hoge JA, Ziolko SK, et al. Kinetic modeling of amyloid binding in humans using PET imaging and Pittsburgh Compound-B. J Cereb Blood Flow Metab. 2005;25:1528–47. doi:10.1038/sj.jcbfm.9600146.
29. Cselenyi Z, Jonhagen ME, Forsberg A, Halldin C, Julin P, Schou M, et al. Clinical validation of F-18-AZD4694, an amyloid-beta-specific PET radioligand. J Nucl Med. 2012;53:415–24. doi:10.2967/jnumed.111.094029.
30. Ito H, Shimada H, Shinotoh H, Takano H, Sasaki T, Nogami T, et al. Quantitative analysis of amyloid deposition in Alzheimer disease using PET and the radiotracer C-11-AZD2184. J Nucl Med. 2014;55:932–8. doi:10.2967/jnumed.113.133793.
31. Falany CN, Krasnykh V, Falany JL. Bacterial expression and characterization of a cDNA for human liver estrogen sulfotransferase. J Steroid Biochem Mol Biol. 1995;52:529–39.
32. Mathis CA, Holt D, Wang YM, Huang GF, Debnath M, Shao L, et al. Species-dependent formation and identification of the brain metabolites of the amyloid imaging agent [C-11]PIB. Neurobiol Aging. 2004;25:S277–S8. doi:10.1016/S0197-4580(04)80924-2.