title: Florbetapir (18F), a PET imaging agent that binds to amyloid plaques for the potential detection of Alzheimer's disease.
abstract: Florbetapir (18F), being developed by Avid Radiopharmaceuticals, is an 18F-labeled PET tracer binding to amyloid-β (Aβ) plaques for the potential detection of Alzheimer's disease (AD). Preclinical studies indicated high binding affinity of florbetapir (18F) to Aβ fibrils and specific labeling of Aβ plaques in the cortical regions and hippocampus. In phase I and II clinical trials, florbetapir (18F) clearly differentiated patients with AD from healthy controls and uptake was most prominent in the precuneus. The neocortical-to-cerebellar tracer uptake ratio reached a plateau within 50 min post-injection and high-quality images were acquired with 5 to 10 min image acquisition time with 370 MBq of florbetapir (18F). Results from an ongoing phase III clinical trial confirmed a strong correlation between florbetapir (18F) PET images and postmortem assessment of Aβ deposition. No serious adverse events were reported in any of the clinical trials of florbetapir (18F). At the time of publication, a marketing application for florbetapir (18F) had been submitted to the US FDA. The fast kinetics and strong evidences of radiological-pathological correlation are advantages of florbetapir (18F) over other 18F-labeled amyloid PET tracers. This tracer has a potential to serve as an agent for preclinical detection of AD-related pathology in the large elderly population.
authors.affiliation: Tohoku University School of Medicine, Department of Pharmacology, 2-1, Seiryo-machi, Aoba-ku, Sendai 9808575, Japan. nookamura@med.tohoku.ac.jp
authors.forename: Nobuyuki
authors.initials: N
authors.lastname: Okamura
authors.forename: Kazuhiko
authors.initials: K
authors.lastname: Yanai
mesh_terms: D000544:Alzheimer Disease / Q000000981:diagnostic imaging*; D000814:Aniline Compounds / Q000009:adverse effects / Q000493:pharmacokinetics; D000818:Animals; D001921:Brain / Q000000981:diagnostic imaging*; D005026:Ethylene Glycols / Q000009:adverse effects / Q000493:pharmacokinetics; D005462:Fluorine Radioisotopes / Q000009:adverse effects / Q000493:pharmacokinetics; D006801:Humans; D057054:Molecular Imaging; D058225:Plaque, Amyloid / Q000000981:diagnostic imaging*; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000009:adverse effects / Q000493:pharmacokinetics
chemical_list: D000814:Aniline Compounds; D005026:Ethylene Glycols; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; C545186:florbetapir