Heurling Kerstin, Leuzy Antoine, Zimmer Eduardo R, Lubberink Mark, Nordberg Agneta
Section of Nuclear Medicine and PET, Department of Surgical Sciences, Uppsala University, Uppsala, Sweden.
Department NVS, Centre for Alzheimer Research, Division of Translational Alzheimer Neurobiology, Karolinska Institutet, Huddinge, Sweden.
Eur J Nucl Med Mol Imaging. 2016 Feb;43(2):362-373. doi: 10.1007/s00259-015-3208-1. Epub 2015 Oct 6.
In Alzheimer's disease (AD), the deposition of β-amyloid (Aβ) is hypothesized to result in a series of secondary neurodegenerative processes, leading ultimately to synaptic dysfunction and neuronal loss. Since the advent of the first Aβ-specific positron emission tomography (PET) ligand, (11)C-Pittsburgh compound B ([(11)C]PIB), several (18)F ligands have been developed that circumvent the limitations of [(11)C]PIB tied to its short half-life. To date, three such compounds have been approved for clinical use by the US and European regulatory bodies, including [(18)F]AV-45 ([(18)F]florbetapir; Amyvid™), [(18)F]-BAY94-9172 ([(18)F]florbetaben; Neuraceq™) and [(18)F]3'-F-PIB ([(18)F]flutemetamol; Vizamyl™). The present review aims to summarize and discuss the currently available knowledge on [(18)F]flutemetamol PET. As the (18)F analogue of [(11)C]PIB, [(18)F]flutemetamol may be of use in the differentiation of AD from related neurodegenerative disorders and may help with subject selection and measurement of target engagement in the context of clinical trials testing anti-amyloid therapeutics. We will also discuss its potential use in non-AD amyloidopathies.
在阿尔茨海默病(AD)中,β-淀粉样蛋白(Aβ)的沉积被认为会引发一系列继发性神经退行性过程,最终导致突触功能障碍和神经元丧失。自首个Aβ特异性正电子发射断层扫描(PET)配体——(11)C-匹兹堡化合物B([(11)C]PIB)问世以来,已经开发出几种(18)F配体,克服了[(11)C]PIB因其半衰期短所带来的局限性。迄今为止,已有三种此类化合物获得美国和欧洲和欧洲监管机构批准用于临床,包括[(18)F]AV-45([(18)F]氟比他派;Amyvid™)、[(18)F]-BAY94-9172([(18)F]氟比他班;Neuraceq™)和[(18)F]3'-F-PIB([(18)F]氟代美他莫;Vizamyl™)。本综述旨在总结和讨论目前关于[(18)F]氟代美他莫PET的现有知识。作为[(11)C]PIB的(18)F类似物,[(18)F]氟代美他莫可能有助于区分AD与相关神经退行性疾病,并且在测试抗淀粉样蛋白疗法的临床试验中,可能有助于受试者的选择以及靶点结合情况的测量。我们还将讨论其在非AD淀粉样变性病中的潜在用途。