Journal Article 18F-FPYBF-2, a new F-18-labelled amyloid imaging PET tracer: first experience in 61 volunteers and 55 patients with dementia

Higashi, Tatsuya  ,  Nishii, Ryuichi  ,  Kagawa, Shinya  ,  Kishibe, Yoshihiko  ,  Takahashi, Masaaki  ,  Okina, Tomoko  ,  Suzuki, Norio  ,  Hasegawa, Hiroshi  ,  Nagahama, Yasuhiro  ,  Ishizu, Koichi  ,  Oishi, Naoya  ,  Kimura, Hiroyuki  ,  Watanabe, Hiroyuki  ,  Ono, Masahiro  ,  Saji, Hideo  ,  Yamauchi, Hiroshi

2018-01 , Springer Japan
Objective: Recently, we developed a benzofuran derivative for the imaging of β-amyloid plaques, 5-(5-(2-(2-(2-18F-fluoroethoxy)ethoxy)ethoxy)benzofuran-2-yl)- Nmethylpyridin-2-amine (18F-FPYBF-2) (Ono et al., 2011). The aim of this study was toassess the feasibility of 18F-FPYBF-2 as an amyloid imaging PET tracer in a firstclinical study with healthy volunteers and patients with various dementia and incomparative dual tracer study using 11C-Pittsburgh Compound B (11C-PiB).Methods: Sixty-one healthy volunteers (age: 53.7+/-13.1 y.o.; 19 male and 42 female;age range 24-79) and fifty-five patients with suspected dementia (Alzheimer's Disease(AD); early AD: n=19 and moderate stage AD: n=8, other dementia: n=9, MildCognitive Impairment; MCI: n=16, cognitively normal: n=3) for first clinical studyunderwent static head PET/CT scan using 18F-FPYBF-2 at 50-70min after injection.Thirteen volunteers and fourteen patients also underwent dynamic PET scan at 0-50min at the same instant. Sixteen subjects (volunteers: n=5, patients with dementia:n=11) (age: 66.3+/-14.2 y.o.; 10 male and 6 female) were evaluated for comparativestudy (50-70min after injection) using 18F-FPYBF-2 and 11C-PiB on separate days,respectively. Quantitative analysis of mean cortical uptake was calculated using MeanCortical Index of SUVR (Standardized Uptake Value Ratio) based on the establishedmethod for 11C-PiB analysis using cerebellar cortex as control.Results: Studies with healthy volunteers showed that 18F-FPYBF-2 uptake was mainlyobserved in cerebral white matter and that average Mean Cortical Index at 50-70minwas low and stable (1.066+/-0.069) basically independent from age or gender. Inpatients with AD, 18F-FPYBF-2 uptake was observed both in cerebral white and graymatter and Mean Cortical Index was significantly higher (early AD: 1.288+/-0.134,moderate AD: 1.342+/-0.191) than those of volunteers and other dementia (1.018+/-0.057). In comparative study, the results of 18F-FPYBF-2 PET/CT were comparablewith those of 11C-PiB, and the Mean Cortical Index (18F-FPYBF-2: 1.173+/-0.215;11C-PiB: 1.435+/-0.474) showed direct proportional relationship with each other(p<0.0001).Conclusions: Our first clinical study suggest that 18F-FPYBF-2 is a useful PET tracerfor the evaluation of β-amyloid deposition and that quantitative analysis of MeanCortical Index of SUVR is a reliable diagnostic tool for the diagnosis of AD.

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