@article{oai:repo.qst.go.jp:00048767,
 author = {Higashi, Tatsuya and Nishii, Ryuichi and Kagawa, Shinya and Kishibe, Yoshihiko and Takahashi, Masaaki and Okina, Tomoko and Suzuki, Norio and Hasegawa, Hiroshi and Nagahama, Yasuhiro and Ishizu, Koichi and Oishi, Naoya and Kimura, Hiroyuki and Watanabe, Hiroyuki and Ono, Masahiro and Saji, Hideo and Yamauchi, Hiroshi and 東 達也 and 西井 龍一},
 journal = {Annals of Nuclear Medicine},
 month = {Jan},
 note = {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 to
assess the feasibility of 18F-FPYBF-2 as an amyloid imaging PET tracer in a first
clinical study with healthy volunteers and patients with various dementia and in
comparative 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, Mild
Cognitive Impairment; MCI: n=16, cognitively normal: n=3) for first clinical study
underwent 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 comparative
study (50-70min after injection) using 18F-FPYBF-2 and 11C-PiB on separate days,
respectively. Quantitative analysis of mean cortical uptake was calculated using Mean
Cortical Index of SUVR (Standardized Uptake Value Ratio) based on the established
method for 11C-PiB analysis using cerebellar cortex as control.
Results: Studies with healthy volunteers showed that 18F-FPYBF-2 uptake was mainly
observed in cerebral white matter and that average Mean Cortical Index at 50-70min
was low and stable (1.066+/-0.069) basically independent from age or gender. In
patients with AD, 18F-FPYBF-2 uptake was observed both in cerebral white and gray
matter 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 comparable
with 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 tracer
for the evaluation of β-amyloid deposition and that quantitative analysis of Mean
Cortical Index of SUVR is a reliable diagnostic tool for the diagnosis of AD.},
 title = {18F-FPYBF-2, a new F-18-labelled amyloid imaging PET tracer: first experience in 61 volunteers and 55 patients with dementia},
 volume = {32},
 year = {2018}
}