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Current situation and potential utility of novel PBB3 derivatives: first-in-human PET study with 18F-AM-PBB3 and 18F-PM-PBB3
https://repo.qst.go.jp/records/72709
https://repo.qst.go.jp/records/7270974a27835-17d9-472a-b646-a7fa608fd095
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-03-20 | |||||
| タイトル | ||||||
| タイトル | Current situation and potential utility of novel PBB3 derivatives: first-in-human PET study with 18F-AM-PBB3 and 18F-PM-PBB3 | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_c94f | |||||
| 資源タイプ | conference object | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
島田, 斉
× 島田, 斉× 北村, 聡一郎× 小野, 麻衣子× 島田 斉× 北村 聡一郎× 小野 麻衣子 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Background: Recent advancements of novel tau positron emission tomography (PET) ligands are shedding light on the nature of diverse tauopathies, such as Alzheimer’s disease (AD), primary age-related tauopathy (PART), progressive nuclear palsy (PSP), corticobasal degeneration (CBD), and so on. Affinity and selectivity to distinct tau pathologies depends on each ligand. Our previous studies demonstrated that 11C-pyridinylbutadienyl-benzothiazole 3 (11C-PBB3) can detect a broad range of tau inclusions. However, 11C-PBB3 have several issues including relatively short half-life of 11C, limited dynamic range, metabolic instability and off-target binding around basal ganglia and thalamus, leading to difficulty in wide use and early detection of tau pathologies especially in patients with PSP and CBD. To overcome these drawbacks of 11C-PBB3, we have developed novel PBB3 derivatives, 18F-AM-PBB3 and 18F-PM-PBB3. Aims of the present study are to investigate characteristics of in vivo PET imaging of fluorinated PBB3 derivatives and to explore the potential utility of these ligands. Methods: Participants are four patients with AD and four age-matched cognitive healthy control (HC) subjects for 18F-AM-PBB3 PET scan, and two patient with AD and two HC for 18F-PM-PBB3 PET scan, respectively. Arterial blood sampling, and free fraction measurements after injection of 18F-AM-PBB3 and 18-F-PBB3. 11C-PBB3 and 11C-PiB PET scans were also performed within a month. Parametric 18F-AM-PBB3, 18-F-PBB3, 11C-PBB3 and 11C-PiB images were generated by voxel-based calculation of standard standardized uptake value ratio (SUVR) to the cerebellum. Results: Dynamic ranges of 18F-AM-PBB3 and 18F-PM-PBB3 yields about 1.5 and 2 fold higher than 11C-PBB3 in visualizing AD tau lesions, respectively. Distribution patterns of specific binding are similar among each ligand. Off-target binding of 11C-PBB3 is noticeable in the basal ganglia and thalamus, while 18F-AM-PBB3 and 18F-PM-PBB3 does not produce prominent off-target signals in these areas. Unfortunately, off-target binding to choroid plexus are conspicuous in 18F-PM-PBB3 and slightly noticeable in 18F-AM-PBB3, while 11C-PBB shows little off-target binding. Conclusions: The present study demonstrated that fluorinated PBB3 derivatives showed similar characteristics to 11C-PBB3 with long half-life, broad dynamic range and less off-target binding around the basal ganglia and thalamus. Potential utility of fluorinated PBB3 derivatives in non-AD tauopathies is also expected. |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | Alzheimer's Association International Conference | |||||
| 発表年月日 | ||||||
| 日付 | 2017-07-18 | |||||
| 日付タイプ | Issued | |||||
