Comparison of new tau PET-tracer candidates with [18F]T808 and [18F]T807

Molecular Imaging

Volumn 15, Issue , 2016, Pages 1-15

  Declercq, Lieven ^a   Celen, Sofie ^a   Lecina, Joan ^a   Ahamed, Muneer ^a   Tousseyn, Thomas ^b   Moechars, Diederik ^c   Alcazar, Jesus ^d   Ariza, Manuela ^d   Fierens, Katleen ^d   Bottelbergs, Astrid ^c   Mariën, Jonas ^c   Vandenberghe, Rik ^a   Andres, Ignacio Jose ^d   Van Laere, Koen ^b   Verbruggen, Alfons ^a   Bormans, Guy ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

^b DEPARTMENT OF IMAGING AND PATHOLOGY   (Belgium)

^c JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^d Janssen Cilag EMEA Belgium   (Belgium)

Author keywords

Alzheimer; Biomarker; Molecular imaging of neurodegenerative diseases; PET imaging

Indexed keywords

BINDING ENERGY; BINS; BIOMARKERS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; LIGANDS; LIQUID CHROMATOGRAPHY; MAMMALS; NEURODEGENERATIVE DISEASES; POSITRON EMISSION TOMOGRAPHY; RADIOGRAPHY;

ALZHEIMER; BINDING AFFINITIES; PET IMAGING; RADIOLABELED TRACERS; RADIOMETABOLITE ANALYSIS; SELECTIVE BLOCKING; SELECTIVE INTERACTION; STRUCTURAL REQUIREMENTS;

MOLECULAR IMAGING;

BENZIMIDAZOLE DERIVATIVE; FLUORINE; MAPT PROTEIN, HUMAN; PYRIMIDINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT; T808 COMPOUND; TAU PROTEIN;

ALZHEIMER DISEASE; ANIMAL; BRAIN CHEMISTRY; CHEMISTRY; COMPARATIVE STUDY; DIAGNOSTIC IMAGING; GENETICS; HUMAN; METABOLISM; MOUSE; MUTATION; PLASMA; POSITRON EMISSION TOMOGRAPHY; TISSUE DISTRIBUTION; TRANSGENIC MOUSE;

ALZHEIMER DISEASE; ANIMALS; BENZIMIDAZOLES; BRAIN CHEMISTRY; FLUORINE RADIOISOTOPES; HUMANS; MICE; MICE, TRANSGENIC; MUTATION; PLASMA; POSITRON-EMISSION TOMOGRAPHY; PYRIMIDINES; RADIOPHARMACEUTICALS; TAU PROTEINS; TISSUE DISTRIBUTION;

EID: 85016130019     PISSN: 15353508     EISSN: None     Source Type: Journal    
DOI: 10.1177/1536012115624920     Document Type: Review

References (39)

1. Masters CL, Cappai R, Barnham KJ, et al. Molecular mechanisms for Alzheimer's disease: implications for neuroimaging and therapeutics. J Neurochem. 2006;97(6):1700-1725.
2. Hyman BT, Phelps CH, Beach TG, et al. National Institute on Aging-Alzheimer's Association guidelines for the neuropathologic assessment of Alzheimer's disease. Alzheimers Dement. 2012;8(1): 1-13.
3. Okamura N, Suemoto T, Furumoto S, et al. Quinoline and benzimidazole derivatives: candidate probes for in vivo Imaging of tau pathology in Alzheimer's disease. J Neurosci. 2005;25(47): 10857-10862.
4. Yang L, Rieves D, Ganley C. Brain amyloid imaging-FDA approval of florbetapir F18 injection. N Engl J Med. 2012; 367(10):885-887.
5. Gomez-Isla T, Hollister R, West H, et al. Neuronal loss correlates with but exceeds neurofibrillary tangles in Alzheimer's disease. Ann Neurol. 1997;41(1):17-24.
6. Arriagada PV, Growdon JH, Hedley-Whyte ET, Hyman BT. Neurofibrillary tangles but not senile plaques parallel duration and severity of Alzheimer's disease. Neurology. 1992;42(3 pt 1):631-639.
7. Villemagne VL, Furumoto S, Fodero-Tavoletti M, et al. The challenges of tau imaging. Future Neurol. 2012;7(4):409-421.
8. Zhang W, Arteaga J, Cashion DK, et al. A highly selective and specific PET tracer for imaging of tau pathologies. J Alzheimer's Dis. 2012;31(3):601-612.
9. Spillantini MG, Goedert M. Tau pathology and neurodegeneration. Lancet Neurol. 2013;12(6):609-622.
10. Fodero-Tavoletti MT, Okamura N, Furumoto S, et al. 18FTHK523: a novel in vivo tau imaging ligand for Alzheimer's disease. Brain. 2011;134(pt 4):1089-1100.
11. Xia CF, Arteaga J, Chen G, et al. [(18)F]T807, a novel tau positron emission tomography imaging agent for Alzheimer's disease. Alzheimers Dement. 2013;9(6):666-676.
12. Xia S, Garrett MC, Timothy JD, et al. Evaluation of [11C]N-methyl lansoprazole as a radiopharmaceutical for PET imaging of tau neurofibrillary tangles. ACS Med Chem Lett. 2013;3(11):936-941.
13. Okamura N, Furumoto S, Harada R, et al. Novel 18F-labeled arylquinoline derivatives for noninvasive imaging of tau pathology in Alzheimer disease. J Nucl Med. 2013;54(8):1-8.
14. Maruyama M, Shimada H, Suhara T, et al. Imaging of tau pathology in a tauopathy mouse model and in Alzheimer patients compared to normal controls. Neuron. 2013;79(6):1094-1108.
15. Shah M, Catafau AM. Molecular imaging insights into neurodegeneration: focus on tau PET radiotracers. J Nucl Med. 2014; 55(6):871-874.
16. Villemagne VL, Fodero-Tavoletti MT, Masters CL, Rowe CC. Tau imaging: early progress and future directions. Lancet Neurol. 2015;14(1):114-124.
17. Ariza M, Kolb HC, Moechars D, et al. Tau PET imaging: past, present and future. J Med Chem. 2015;58(11):4365-4382.
18. Chien DT, Bahri S, Szardenings AK, et al. Early clinical PET imaging results with the novel PHF-tau radioligand [F-18]- T807. J Alzheimer's Dis. 2012;34(2):457-468.
19. Chien DT, Szardenings AK, Bahri S, et al. Early clinical PET imaging results with the novel PHF-tau radioligand [F18]-T808. J Alzheimer's Dis. 2013;38(1):171-184.
20. Zimmer ER, Leuzy A, Bhat V, Gauthier S, Rosa-Neto P. In vivo tracking of tau pathology using positron emission tomography (PET) molecular imaging in small animals. Transl Neurodegener. 2014;3(1):6.
21. Szardenings AK, Kolb HC, Walsh JC, et al. Imaging agents for detecting neurological dysfunction. US patent 20120302755 Al 2012.
22. Szardenings AK, Zhang W, Kolb HC, et al. Imaging agents for detecting neurological disorders. US patent 2011/0182812A1 2011.
23. Serdons K, Verduyckt T, Vanderghinste D, et al. Synthesis of 18F-labelled 2-(4′-fluorophenyl)-1,3-benzothiazole and evaluation as amyloid imaging agent in comparison with [11C]PIB. Bioorg Med Chem Lett. 2009;19(3):602-605.
24. Prabhu PP, Shastry CS, Pande SS, et al. Design, synthesis, characterization and biological evaluationof Benzothiazole-6-carboxylate derivatives. Res Pharm. 2011;1(2):6-12.
25. Chimenti F, Bizzarri B, Bolasco A, et al. Synthesis and biological evaluation of novel 2,4-disubstituted-1,3-thiazoles as anti-Candida spp. agents. Eur J Med Chem. 2011;46(1):378-382.
26. Li H, Wang C, Huang H, et al. Silver-catalyzed cascade reaction of o-aminoaryl compounds with alkynes: an aniline mediated synthesis of 2-substituted quinolines. Tetrahedron Lett. 2011; 52(10):1108-1111.
27. Wilson AA, Garcia A, Chestakova A, et al. A rapid one-step radiosynthesis of the b-amyloid imaging radiotracer N-methyl- [11C]2-(40-methylaminophenyl)-6-hydroxybenzothiazole ([11C]-6-OH-BTA-1). J Labelled Compd Radiopharm. 2004; 47(10):679-682.
28. Greenberg SG, Davies P. A preparation of Alzheimer paired helical filaments that displays distinct tau proteins by polyacrylamide gel electrophoresis. Proc Natl Acad Sci U S A. 1990;87(15): 5827-5831.
29. Pike VW. PET radiotracers: crossing the blood-brain barrier and surviving metabolism. Trends Pharmacol Sci. 2009;30(8): 431-440.
30. Braak H, Braak E. Neuropathological stageing of Alzheimerrelated changes. Acta Neuropathol. 1991;82(4):239-259.
31. Marquie M, Normandin MD, Vanderburg CR, et al. Validating novel tau PET tracer [F-18]-AV-1451 (T807) on postmortem brain tissue. Ann Neurol. 2015;78(5):787-800.
32. Rojo LE, Alzate-Morales J, Saavedra IN, et al. Selective interaction of lansoprazole and astemizole with tau polymers: potential new clinical use in diagnosis of Alzheimer's disease. J Alzheimer's Dis. 2010;19(2):573-589.
33. Fawaz MV, Brooks AF, Rodnick ME, et al. High affinity radiopharmaceuticals based upon lansoprazole for PET imaging of aggregated tau in Alzheimer's disease and progressive supranuclear palsy: synthesis, preclinical evaluation, and lead selection. ACS Chem Neurosci. 2014;5(8):718-730.
34. Riss PJ, Brichard L, Ferrari V, et al. Radiosynthesis and characterization of astemizole derivatives as lead compounds toward PET imaging of t-pathology. Med Chem Commun. 2013;4(5): 852-855.
35. Shoghi-Jadid K, Small GW, Agdeppa ED, et al. Localization of neurofibrillary tangles and beta-amyloid plaques in the brains of living patients with Alzheimer disease. Am J Geriatr Psychiatry. 2002;10(1):24-35.
36. Klunk WE, Engler H, Nordberg A, et al. Imaging brain amyloid in Alzheimer's disease with Pittsburgh Compound-B. Ann Neurol. 2004;55(3):306-319.
37. Bulic B, Pickhardt M, Schmidt B. Development of tau aggregation inhibitors for Alzheimer's disease. Angew Chem Int Ed Engl. 2009;48(10):1740-1752.
38. Jensen JR, Cisek K, Honson NS, Kuret J. Ligand polarizability contributes to tau fibril binding affinity. Bioorg Med Chem. 2011; 19(17):5147-5154.
39. Duyckaerts C, Potier MC, Delatour B. Alzheimer disease models and human neuropathology: similarities and differences. Acta Neuropathol. 2008;115(1):5-38.