@misc{oai:repo.qst.go.jp:00072716, author = {島田, 斉 and 島田 斉}, month = {Feb}, note = {Background and Aims: 11C-PBB3 is a tau PET ligand that can visualize diverse tau pathologies including Alzheimer’s disease (AD), non-AD tauopathies, and tau transgenic mice. We have developed a 18F-labeled PBB3 derivative, 18F-PM-PBB3. To evaluate the potential utility of this ligand in clinical trials of tau targeting agents, we conducted preclinical and clinical studies using 18F-PM-PBB3. Methods: Preclinical characterization of 18F-PM-PBB3 was performed using brain samples of humans and model mice. To perform head-to-head comparison between 18F-PM-PBB3 and 11C-PBB3, patients with AD and progressive supranuclear palsy (PSP), and cognitively healthy subjects underwent PET scans with 18F-PM-PBB3 and 11C-PBB3. Results: Preclinical evaluations demonstrated that 18F-PM-PBB3 can bind diverse tau pathologies, including AD, PSP, corticobasal degeneration and Pick’s disease, with high sensitivity and specificity. In clinical PET study, dynamic ranges of 18F-PM-PBB3 yield about 2-fold higher than 11C-PBB3 in visualizing tau lesions, while distribution patterns of specific binding are similar. 18F-PM-PBB3 does not produce prominent off-target signals in basal ganglia. Standardized uptake value ratios can be used as robust and simplified indices of the specific binding. Conclusions: 18F-PM-PBB3 is a promising PET ligand for quantifying tau pathologies in AD and non-AD patients with suitable pharmacokinetics and high contrast., 13th Annual Biomarkers Congress}, title = {Potential utility of novel tau PET ligand, 18F-PM-PBB3}, year = {2017} }