ABSTRACT
The deposition of ß-amyloid (Aß) in the brain is a pathologic hallmark of Alzheimer's disease (AD), appearing years before the onset of symptoms, and its detection is incorporated into clinical diagnosis. Here, we have discovered and developed a class of diaryl-azine derivatives for detecting Aß plaques in the AD brain using PET imaging. After a set of comprehensive preclinical assessments, we screened out a promising Aß-PET tracer, [18F]92, with a high binding affinity to the Aß aggregates, significant binding ability with the AD brain sections, and optimal brain pharmacokinetic properties in rodents and non-human primates. The first-in-human PET study declared that [18F]92 displayed low white matter uptake and could bind to Aß pathology for distinguishing AD from healthy control subjects. All these results support that [18F]92 might become a promising PET tracer for visualizing Aß pathology in AD patients.
Subject(s)
Alzheimer Disease , Amyloid beta-Peptides , Animals , Humans , Amyloid beta-Peptides/metabolism , Alzheimer Disease/diagnostic imaging , Alzheimer Disease/metabolism , Fluorine Radioisotopes/metabolism , Positron-Emission Tomography/methods , Brain/metabolismABSTRACT
Radiopharmaceuticals are essential components of nuclear medicine and serve as one of the cornerstones of molecular imaging and precision medicine. They provide new means and approaches for early diagnosis and treatment of diseases. After decades of development and hard efforts, a relatively matured radiopharmaceutical production and management system has been established in China with high-quality facilities. This review provides an overview of the current status of radiopharmaceuticals on production and distribution, clinical application, and regulatory supervision and also describes some important advances in research and development and clinical translation of radiopharmaceuticals in the past 10 years. Moreover, some prospects of research and development of radiopharmaceuticals in the near future are discussed.
