Journal Article

Evaluation of a novel PET tracer 18F-Florbetazine for Alzheimer's disease diagnosis and β-amyloid deposition quantification

Ge, Qi, Ren, Chao, Huang, Zhenghai, Huo, Li, Mao, Chenhui, Zhang, Haiqiong, Yan, Mengshi, Wu, Meiqi, Li, Bo, Li, Yuying, Feng, Feng, Wu, Runze, Gao, Jing, Cui, Mengchao, Dong, Liling, Yang, Xueqian

2024

Overview

•The novel Aβ-targeted PET radioligand [18F]-Florbetazine had distinct binding profiles in AD patients and healthy controls in the dynamic PET study.•[18F]-Florbetazine PET show high gray-to-white contrast in AD patients that are favorable in visual read.•SUVR of a static [18F]-Florbetazine PET scan can be used to differentiated HCs and AD patients. [18F]-Florbetazine ([18F]-92) is a selective PET tracer for β-amyloid (Aβ) depositions with a novel diaryl-azine scaffold to reduce lipophilicity and to achieve higher gray-to-white matter contrast. We aimed to assess its diagnostic value in Alzheimer's disease (AD) and pharmacokinetics characteristics in human subjects. Six healthy controls (HCs) and nine AD patients underwent dynamic PET examination with [18F]-Florbetazine and a structural MRI scan. The time-activity-curves (TACs) for volumes of interest (VOIs) in cerebral cortex, cerebellar cortex and cerebral white matter was depicted and their standardized uptake value ratios (SUVRs) with cerebellar cortex as reference were compared between HCs and AD patients. The cerebral gray-to-white matter SUV ratio (GWR) was also calculated. In HCs, radioactivities in the cerebral cortex VOIs were homogeneously low and at the same level as in cerebellar cortex, while in AD patients, cortical VOIs expected to contain Aβ exhibited high radioactivity. Cerebral cortex SUVRs remain relatively low in HCs while keep increasing along with time in AD patients. After 15 min, the cerebral cortex SUVRs became significant higher in AD patients compared to HCs with 100 % discrimination accuracy. In AD patients, GWR remained over 1.3 for all time intervals and visual inspection showed lower uptake in cerebral white matter compared to cerebral cortex. [18F]-Florbetazine PET showed high uptake on Aβ plaques and high gray-to-white contrast in AD patients that are favorable in visual read. [18F]-Florbetazine can be potentially used for detection and quantification of Aβ depositions in the living human brain. [Display omitted]

• Publisher: Elsevier Inc,Elsevier Limited,Elsevier
• Subject: [18F]-92 / [18F]-Florbetazine / Aged / Aged, 80 and over / Alzheimer Disease - diagnostic imaging / Alzheimer Disease - metabolism / Alzheimer's disease / Amyloid beta-Peptides - metabolism / Aniline Compounds - pharmacokinetics / Brain - diagnostic imaging / Brain - metabolism / Cerebellum / Cerebral cortex / Data analysis / Dementia / Dynamic PET / Ethylene Glycols - pharmacokinetics / Female / Fluorine Radioisotopes - pharmacokinetics / Humans / Magnetic Resonance Imaging - methods / Male / Middle Aged / Neurodegenerative diseases / Patients / PET/CT / Pharmacokinetics / Positron-Emission Tomography - methods / Radioactivity / Radiopharmaceuticals - pharmacokinetics / Senile plaques / Software / Statistical analysis / Substantia alba / Tetrabenazine - analogs & derivatives / Visual discrimination / β-Amyloid