Presentation Abstract

Session: Imaging Posters
Saturday, Jul 10, 2010, 11:15 AM - 1:15 PM
Presentation: IC-P-121 - Inter-ethnic comparability of pharmacokinetics of Florbetaben (BAY 94-9172), a ß-amyloid imaging PET agent, as a basis of global development of a diagnostics for Alzheimer’s disease
Pres. Time: Saturday, Jul 10, 2010, 11:15 AM -12:15 PM
Location: 313-C
Category: +New imaging methods
Author(s): Michio Senda1, Tomohiko Yamane1, Masahiro Sasaki1, Keiji Shimizu1, Henryk Barthel2, Bernhard Sattler2, Marianne Patt2, Toshiki Nagasawa3, Marcus Schultze-Mosgau3, Yasuko Aitoku3, Osama Sabri2.
1Institute of Biomedical Research and Innovation, Kobe, Japan, 2University of Leipzig, Leipzig, Germany, 3Bayer Healthcare, Berlin, Germany.
Abstract: Background:
Florbetaben (BAY 94-9172) is an F-18 labeled PET imaging agent under development and is a promising diagnostics for Alzheimer’s disease as it binds to brain Aß deposition. The brain uptake of Florbetaben is also influenced by the plasma concentration (pharmacokinetics), which is a function of whole body distribution, metabolism and excretion, and may have a racial difference. To facilitate global development of Florbetaben, the difference in the pharmacokinetics was analyzed and compared between German and Japanese normal subjects.
Phase I trials of Florbetaben were conducted on German and Japanese healthy volunteers, each in 18 subjects, to evaluate and compare the pharmacokinetics and safety of a single dose of 300MBq 18F-florbetaben, either of low (≤ 5 µg, LD) or high (50-55 µg, HD) mass dose. Pharmacokinetic parameters were evaluated based on the total 18F-radioactivity in plasma followed by analysis of the metabolite profile within the frequently drawn blood samples using radio-HPLC.
A rapid elimination of Florbetaben was observed in plasma for both ethnic groups. The dose-normalized area-under-curve (AUC/D) of the unchanged plasma 18F-florbetaben was comparable between LD and HD as well as between Germans (LD: 0.38 min/L, HD: 0.55 min/L) and Japanese (LD: 0.35min/L, HD: 0.45min/L), suggesting inter-ethnic comparability and dose proportionality in florbetaben pharmacokinetics of up to the high mass dose. The AUC/D was not associated with body weight or sex. A polar metabolite fraction was the main radiolabeled degradation product in the plasma radioactivity, which was also comparable between the two different mass doses and between the ethnic groups. Approximately 27-36% of the administered radioactivity was excreted with urine up to 5-12 hours post injection as polar metabolites without any difference between mass doses or ethnic groups. The most frequent adverse effects were mild irritations in the administration site and general complaints, and no signs of safety concern were observed.
There were no significant differences in the pharmacokinetics of 18F-florbetaben in Germans and Japanese, which warrants further global development of the diagnostics.
Disclosures:   M. Senda, Bayer Healthcare; T. Yamane, None; M. Sasaki, Micron Inc; K. Shimizu, None; H. Barthel, Bayer Healthcare; B. Sattler, Bayer Healthcare; M. Patt, Bayer Healthcare; T. Nagasawa, Bayer Healthcare; M. Schultze-Mosgau, Bayer Healthcare; Y. Aitoku, Bayer Healthcare; O. Sabri, Bayer Healthcare; Bayer Healthcare.
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