Authors:
M. Patt University of Leipzig Department of Nuclear Medicine Liebigstr 18 04103 Leipzig Germany

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A. Schildan University of Leipzig Department of Nuclear Medicine Liebigstr 18 04103 Leipzig Germany

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H. Barthel University of Leipzig Department of Nuclear Medicine Liebigstr 18 04103 Leipzig Germany

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G. Becker University of Leipzig Department of Nuclear Medicine Liebigstr 18 04103 Leipzig Germany

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M. Schultze-Mosgau Bayer Schering Pharma AG Berlin Germany

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B. Rohde Bayer Schering Pharma AG Berlin Germany

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C. Reininger Bayer Schering Pharma AG Berlin Germany

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O. Sabri University of Leipzig Department of Nuclear Medicine Liebigstr 18 04103 Leipzig Germany

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Abstract  

[18F]Florbetaben ([18F]BAY 94-9172) is a promising β-amyloid (Aβ) targeted PET-tracer currently in late stage clinical development. [18F]Florbetaben can assist in the more accurate diagnosis of Alzheimer’s Disease (AD) by non-invasive, in vivo detection of Aβ in the brain. To determine the arterial input function of the PET tracer—as part of a proof of mechanism (PoM) study—arterial samples were drawn from all subjects at predefined time points post injection (p.i.), and the proportion of unchanged tracer [18F]Florbetaben was determined by HPLC analysis. Plasma metabolite profiles were investigated following intravenous administration of 300 MBq (±60 MBq) of [18F]Florbetaben to both, patients with AD and healthy controls (HCs), and various methods for processing the blood samples were evaluated. Addition of acetonitrile to plasma samples (obtained from whole blood by centrifugation) and precipitation of proteins resulted in a recovery of more than 90% of the initial radioactivity in the supernatants. High Performance Liquid Chromatography using a polymer-based column (PRP-1) in conjunction with gradient elution was found to be a suitable method of metabolite analysis of [18F]Florbetaben. HPLC analyses indicated that [18F]Florbetaben is rapidly metabolized in vivo with an estimated initial half-life of about 6 min. A polar metabolite fraction, consisting presumably of more than one component, and (to a smaller extent) of the demethylated derivative of [18F]Florbetaben were time-dependently detected in plasma.

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Journal of Radionalytical and Nuclear Chemistry
Language English
Size A4
Year of
Foundation
1968
Volumes
per Year
1
Issues
per Year
12
Founder Akadémiai Kiadó
Founder's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
Publisher's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible
Publisher
Chief Executive Officer, Akadémiai Kiadó
ISSN 0236-5731 (Print)
ISSN 1588-2780 (Online)