title: Ethnic comparison of pharmacokinetics of (18)F-florbetaben, a PET tracer for beta-amyloid imaging, in healthy Caucasian and Japanese subjects.
abstract: OBJECTIVE
  (18)F-Florbetaben is a positron emission tomography (PET) tracer indicated for imaging cerebral beta-amyloid deposition in adult patients with cognitive impairment who are being evaluated for Alzheimer's disease and other causes of cognitive decline. The present study examined ethnic comparability of the plasma pharmacokinetics, which is the input to the brain, between Caucasian and Japanese subjects.
  
  
  METHODS
  Two identical phase I trials were performed in 18 German and 18 Japanese healthy volunteers to evaluate the plasma pharmacokinetics of a single dose of 300 MBq (18)F-florbetaben, either of low (≤5 μg, LD) or high (50-55 μg, HD) mass dose. Pharmacokinetic parameters were evaluated based on the total (18)F radioactivity measurements in plasma followed by metabolite analysis using radio-HPLC.
  
  
  RESULTS
  The pharmacokinetics of (18)F-florbetaben was characterized by a rapid elimination from plasma. The dose-normalized areas under the curve of (18)F-florbetaben in plasma as an indicator of the input to the brain were comparable between Germans (LD: 0.38 min/l, HD: 0.55 min/l) and Japanese (LD: 0.35 min/l, HD: 0.45 min/l) suggesting ethnic similarity, and the mass dose effect was minimal. A polar metabolite fraction was the main radiolabelled degradation product in plasma and was also similar between the doses and the ethnic groups.
  
  
  CONCLUSIONS
  Absence of a difference in the pharmacokinetics of (18)F-florbetaben in Germans and Japanese has warranted further global development of the PET imaging agent.
authors.affiliation: Division of Molecular Imaging, Institute of Biomedical Research and Innovation, 2-2 Minatojima-Minamimachi, Chuo-ku, Kobe, 650-0047, Japan, senda@fbri.org.
authors.forename: Michio
authors.initials: M
authors.lastname: Senda
authors.forename: Masahiro
authors.initials: M
authors.lastname: Sasaki
authors.forename: Tomohiko
authors.initials: T
authors.lastname: Yamane
authors.forename: Keiji
authors.initials: K
authors.lastname: Shimizu
authors.forename: Marianne
authors.initials: M
authors.lastname: Patt
authors.forename: Henryk
authors.initials: H
authors.lastname: Barthel
authors.forename: Bernhard
authors.initials: B
authors.lastname: Sattler
authors.forename: Toshiki
authors.initials: T
authors.lastname: Nagasawa
authors.forename: Marcus
authors.initials: M
authors.lastname: Schultze-Mosgau
authors.forename: Yasuko
authors.initials: Y
authors.lastname: Aitoku
authors.forename: Ludger
authors.initials: L
authors.lastname: Dinkelborg
authors.forename: Osama
authors.initials: O
authors.lastname: Sabri
mesh_terms: D000368:Aged; D000814:Aniline Compounds / Q000097:blood* / Q000652:urine; D044466:Asian People; D005260:Female; D064368:Healthy Volunteers; D006801:Humans; D007564:Japan; D008297:Male; D008875:Middle Aged; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000097:blood* / Q000652:urine; D013267:Stilbenes / Q000097:blood* / Q000652:urine; D044465:White People
chemical_list: D000814:Aniline Compounds; D019275:Radiopharmaceuticals; D013267:Stilbenes; C527756:4-(N-methylamino)-4'-(2-(2-(2-fluoroethoxy)ethoxy)ethoxy)stilbene