MK-6240 Articles – Cerveau Technologies

Characterization of MK6240, a tau PET tracer, in autopsy brain tissue from Alzheimer’s disease cases

Koole M, Lohith TG, Valentine JL, et al. Preclinical safety evaluation and human dosimetry of [18F]MK-6240, a novel PET tracer for imaging neurofibrillary tangles. Mol Imaging Biol. 2020; 22(1):173-180. Doi: 10.1007/s11307-019-01367-w.

Laffon E, Buj S, de Clermont H, Marthan R. Fitting of late dynamic [18F]MK6240 PET scans for in vivo tau quantification. Eur J Nucl Med Mol Imaging. 2020; 47(1):7-8. Doi: 10.1007/s00259-019-04542-x.

Luchsinger JA, Palta P, Rippon B, et al. Sex differences in in vivo Alzheimer’s disease neuropathy in late middle-aged Hispanics. J Alzheimers Dis. 2020; 74(4):1243-1252. Doi: 10.3233/JAD-191183.

Lussier FZ, Pascoal TA, Chamoun M, et al. Mild behavioral impairment is associated with β -amyloid but not tau or neurodegeneration in cognitively intact elderly individuals. Alzheimers Dement. 2020; 16(1):192-199. Doi: 10.1002/alz.12007.

McCluskey SP, Plisson C, Rabiner EA, Howes O. Advances in CNS PET: The state-of-the-art for new imaging targets for pathophysiology and drug development. Eur J Nucl Med Mol Imaging. 2020; 47(2):451-489. Doi: 10.1007/s00259-019-04488-0.

Therriault J, Benedet AL, Pascoal TA, et al. APOEε4 potentiates the relationship between amyloid-β and tau pathologies. Mol Psychiatry. 2020; [Epub ahead of print]. Doi: 10.101038/s41380-020-0688-6.

Zou J, Tao S, Johnson A, et al. Microglial activation, but not tau pathology, is independently associated with amyloid positivity and memory impairment. Neurobiol Aging. 2020; 85:11-21. Doi: 10.1016/j.neurobiolaging.2019.09.019.

Aguero C, Dhaynaut M, Normandin MD, et al. Autoradiography validation of novel tau PET tracer [F-18]-MK-6240 on human postmortem brain tissue. Acta Neuropathol Commun. 2019; 7(1):37. Doi: 10.1186/s40478-019-0686-6.

Devanand DP, Andrews H, Kreisl WC, et al. Antiviral therapy: Valacyclovir Treatment of Alzheimer’s Disease (VALAD) Trial: Protocol for a randomized, double-blind, placebo-controlled, treatment trial. BMJ Open. 2020; 10(2):e032112. Doi: 10.1136/bmjopen-2019-032112.

Murugan NA, Chiotis K, Rodriguez-Vieitez E, Lemoine L, Agren H, Nordberg A. Cross-interaction of tau PET tracers with monoamine oxidase B: Evidence from in silico modelling and in vivo imaging. Eur J Nucl Med Mol Imaging. 2019; 46(6):1369-1382. Doi: 10.1007/s00259-019-04305-8.

Leuzy A, Chiotis K, Lemoine L, et al. Tau PET imaging in neurodegenerative tauopathies – still a challenge. Mol Psychiatry. 2019; 24(8):1112-1134. Doi: 10.1038/s41380-018-0342-8.

Lohith TG, Bennacef I, Vandenberghe R, et al. Brain imaging of Alzheimer dementia patients and elderly controls with 18F-MK-6240, a PET tracer targeting neurofibrillary tangle pathology. J Nucl Med. 2019; 60(1):107-114. Doi: 10.2967/jnumed.118.208215.

Betthauser TJ, Cody KA, Zammit MD, et al. In vivo characterization and quantification of neurofibrillary tau PET radioligand MK-6240 in humans from Alzheimer’s disease dementia to young controls. J Nucl Med. 2019; 60(1):93-99. Doi: 10.2967/jnumed.118.209650.

Guehl NJ, Wooten DW, Yokell DL, et al. Evaluation of pharmacokinetic modeling strategies for in-vivo quantification of tau with the radiotracer [18F]MK6240 in human subjects. Eur J Nucl Med Mol Imaging. 2019; 46(10):2099-2111. Doi: 10.1007/s00259-019-04419-z.

Hopewell R, Ross K, Kostikov A, et al. A simplified radiosynthesis of [18F]MK-6240 for tau PET imaging. J Labelled Comp Radiopharm. 2019; 62(2):109-114. Doi: 10.1002/jlcr.3695.

Salinas C, Lohith TG, Purohit A, et al. Test-retest characteristic of [18F]MK-6240 quantitative outcomes in cognitively normal adults and subjects with Alzheimer’s disease. J Cereb Blood Flow Metab. 2019; [Epub ahead of print]. Doi: 10.1177/0271678X19887781.

Tago T, Toyohara J, Harada R, et al. Characterization of the binding of tau imaging ligands to melanin-containing cells: Putative off-target-binding site. Ann Nucl Med. 2019; 33(6):375-382. Doi: 10.1007/s12149-019-01344-x.

Murugan NA, Nordberg A, Agren H. Different positron emission tomography tau tracers bind to multiple binding sites on the tau fibril: Insight from computational modeling. ACS Chem Neurosci. 2018; 9(7):1757-1767. Doi: 10.1021/acschemneuro.8b00093.

Okamura N, Harada R, Ishiki A, et al. The development and validation of tau PET tracers: Current status and future directions. Clin Transl Imaging. 2018; 6(4):305-316. Doi: 10.1007/s40336-018-0290-y.

Pascoal TA, Shin M, Kang MS, et al. In vivo quantification of neurofibrillary tangles with [18F]MK-6240. Alzheimers Res Ther. 2018; 10(1):1-14. Doi: 10.1186/s13195-018-0402-y.

Collier TL, Yokell DL, Livni E, et al. cGMP production of the radiopharmaceutical [18F]MK-6240 for PET imaging of human neurofibrillary tangles. J Labelled Comp Radiopharm. 2017; 60(5):263-269. Doi: 10.1002/jlcr.3496.

Hostetler ED, Walji AM, Zeng Z, et al. Preclinical characterization of 18F-MK-6240, a promising PET tracer for in vivo quantification of human neurofibrillary tangles. J Nucl Med. 2016; 57(10):1599-1606.

Walji AM, Hostetler ED, Selnick H, et al. Discovery of 6-(fluoro-(18)F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([(18)F]-MK-6240): A positron emission tomography (PET) imaging agent for quantification of neurofibrillary tangles (NFTs). J Med Chem. 2016; 59(10):4778-89. Doi: 10.1021/acs.jmedchem.6b00166.

Categories: MK-6240 Articles

Characterization of MK6240, a tau PET tracer, in autopsy brain tissue from Alzheimer’s disease cases

Timing is everything: tau imaging across stages of Alzheimer’s disease

Koole M, Lohith TG, Valentine JL, et al. Preclinical safety evaluation and human dosimetry of [18F]MK-6240, a novel PET tracer for imaging neurofibrillary tangles. Mol Imaging Biol. 2020; 22(1):173-180. Doi: 10.1007/s11307-019-01367-w.

Laffon E, Buj S, de Clermont H, Marthan R. Fitting of late dynamic [18F]MK6240 PET scans for in vivo tau quantification. Eur J Nucl Med Mol Imaging. 2020; 47(1):7-8. Doi: 10.1007/s00259-019-04542-x.

Luchsinger JA, Palta P, Rippon B, et al. Sex differences in in vivo Alzheimer’s disease neuropathy in late middle-aged Hispanics. J Alzheimers Dis. 2020; 74(4):1243-1252. Doi: 10.3233/JAD-191183.

Lussier FZ, Pascoal TA, Chamoun M, et al. Mild behavioral impairment is associated with β -amyloid but not tau or neurodegeneration in cognitively intact elderly individuals. Alzheimers Dement. 2020; 16(1):192-199. Doi: 10.1002/alz.12007.

McCluskey SP, Plisson C, Rabiner EA, Howes O. Advances in CNS PET: The state-of-the-art for new imaging targets for pathophysiology and drug development. Eur J Nucl Med Mol Imaging. 2020; 47(2):451-489. Doi: 10.1007/s00259-019-04488-0.

Therriault J, Benedet AL, Pascoal TA, et al. APOEε4 potentiates the relationship between amyloid-β and tau pathologies. Mol Psychiatry. 2020; [Epub ahead of print]. Doi: 10.101038/s41380-020-0688-6.

Zou J, Tao S, Johnson A, et al. Microglial activation, but not tau pathology, is independently associated with amyloid positivity and memory impairment. Neurobiol Aging. 2020; 85:11-21. Doi: 10.1016/j.neurobiolaging.2019.09.019.

Aguero C, Dhaynaut M, Normandin MD, et al. Autoradiography validation of novel tau PET tracer [F-18]-MK-6240 on human postmortem brain tissue. Acta Neuropathol Commun. 2019; 7(1):37. Doi: 10.1186/s40478-019-0686-6.

Devanand DP, Andrews H, Kreisl WC, et al. Antiviral therapy: Valacyclovir Treatment of Alzheimer’s Disease (VALAD) Trial: Protocol for a randomized, double-blind, placebo-controlled, treatment trial. BMJ Open. 2020; 10(2):e032112. Doi: 10.1136/bmjopen-2019-032112.

Murugan NA, Chiotis K, Rodriguez-Vieitez E, Lemoine L, Agren H, Nordberg A. Cross-interaction of tau PET tracers with monoamine oxidase B: Evidence from in silico modelling and in vivo imaging. Eur J Nucl Med Mol Imaging. 2019; 46(6):1369-1382. Doi: 10.1007/s00259-019-04305-8.

Leuzy A, Chiotis K, Lemoine L, et al. Tau PET imaging in neurodegenerative tauopathies – still a challenge. Mol Psychiatry. 2019; 24(8):1112-1134. Doi: 10.1038/s41380-018-0342-8.

Lohith TG, Bennacef I, Vandenberghe R, et al. Brain imaging of Alzheimer dementia patients and elderly controls with 18F-MK-6240, a PET tracer targeting neurofibrillary tangle pathology. J Nucl Med. 2019; 60(1):107-114. Doi: 10.2967/jnumed.118.208215.

Betthauser TJ, Cody KA, Zammit MD, et al. In vivo characterization and quantification of neurofibrillary tau PET radioligand MK-6240 in humans from Alzheimer’s disease dementia to young controls. J Nucl Med. 2019; 60(1):93-99. Doi: 10.2967/jnumed.118.209650.

Guehl NJ, Wooten DW, Yokell DL, et al. Evaluation of pharmacokinetic modeling strategies for in-vivo quantification of tau with the radiotracer [18F]MK6240 in human subjects. Eur J Nucl Med Mol Imaging. 2019; 46(10):2099-2111. Doi: 10.1007/s00259-019-04419-z.

Hopewell R, Ross K, Kostikov A, et al. A simplified radiosynthesis of [18F]MK-6240 for tau PET imaging. J Labelled Comp Radiopharm. 2019; 62(2):109-114. Doi: 10.1002/jlcr.3695.

Salinas C, Lohith TG, Purohit A, et al. Test-retest characteristic of [18F]MK-6240 quantitative outcomes in cognitively normal adults and subjects with Alzheimer’s disease. J Cereb Blood Flow Metab. 2019; [Epub ahead of print]. Doi: 10.1177/0271678X19887781.

Tago T, Toyohara J, Harada R, et al. Characterization of the binding of tau imaging ligands to melanin-containing cells: Putative off-target-binding site. Ann Nucl Med. 2019; 33(6):375-382. Doi: 10.1007/s12149-019-01344-x.

Murugan NA, Nordberg A, Agren H. Different positron emission tomography tau tracers bind to multiple binding sites on the tau fibril: Insight from computational modeling. ACS Chem Neurosci. 2018; 9(7):1757-1767. Doi: 10.1021/acschemneuro.8b00093.

Okamura N, Harada R, Ishiki A, et al. The development and validation of tau PET tracers: Current status and future directions. Clin Transl Imaging. 2018; 6(4):305-316. Doi: 10.1007/s40336-018-0290-y.

Pascoal TA, Shin M, Kang MS, et al. In vivo quantification of neurofibrillary tangles with [18F]MK-6240. Alzheimers Res Ther. 2018; 10(1):1-14. Doi: 10.1186/s13195-018-0402-y.

Collier TL, Yokell DL, Livni E, et al. cGMP production of the radiopharmaceutical [18F]MK-6240 for PET imaging of human neurofibrillary tangles. J Labelled Comp Radiopharm. 2017; 60(5):263-269. Doi: 10.1002/jlcr.3496.

Hostetler ED, Walji AM, Zeng Z, et al. Preclinical characterization of 18F-MK-6240, a promising PET tracer for in vivo quantification of human neurofibrillary tangles. J Nucl Med. 2016; 57(10):1599-1606.