| Budget Amount *help |
¥130,390,000 (Direct Cost: ¥100,300,000、Indirect Cost: ¥30,090,000)
Fiscal Year 2018: ¥23,660,000 (Direct Cost: ¥18,200,000、Indirect Cost: ¥5,460,000)
Fiscal Year 2017: ¥23,660,000 (Direct Cost: ¥18,200,000、Indirect Cost: ¥5,460,000)
Fiscal Year 2016: ¥23,790,000 (Direct Cost: ¥18,300,000、Indirect Cost: ¥5,490,000)
Fiscal Year 2015: ¥23,660,000 (Direct Cost: ¥18,200,000、Indirect Cost: ¥5,460,000)
Fiscal Year 2014: ¥35,620,000 (Direct Cost: ¥27,400,000、Indirect Cost: ¥8,220,000)
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| Outline of Final Research Achievements |
We performed the investigation of clinical utility of [18F]THK-5351 in neurodegenerative diseases such as tauopathies and validation studies of PET images such as imaging-pathology correlations. Recent validation studies revealed that dominant off-target substrate of [18F]THK-5351 was monoamine oxidase-B (MAO-B), suggesting that [18F]THK-5351 PET has limited utility for selective detection of tau pathology.The aim of study was to develop next generation of selective tau PET tracers, which showed no off-target binding. We synthesized about 200 compounds and screened using the binding assay for tau aggregates from AD and recombinant MAO-B. After identifying candidates for further evaluation of F-18 labeled compounds, we performed in vitro autoradiography using human brain tissues, led to the discovery of F-18 labeled compounds, a promising tau PET tracer candidate that was shown to have a selective binding profile to tau without off-target binding and suitable pharmacokinetics.
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