title: GMP-compliant automated synthesis of [(18)F]AV-45 (Florbetapir F 18) for imaging beta-amyloid plaques in human brain.
abstract: We report herein the Good Manufacturing Practice (GMP)-compliant automated synthesis of (18)F-labeled styrylpyridine, AV-45 (Florbetapir), a novel tracer for positron emission tomography (PET) imaging of beta-amyloid (Abeta) plaques in the brain of Alzheimer's disease patients. [(18)F]AV-45 was prepared in 105 min using a tosylate precursor with Sumitomo modules for radiosynthesis under GMP-compliant conditions. The overall yield was 25.4+/-7.7% with a final radiochemical purity of 95.3+/-2.2% (n=19). The specific activity of [(18)F]AV-45 reached as high as 470+/-135 TBq/mmol (n=19). The present studies show that [(18)F]AV-45 can be manufactured under GMP-compliant conditions and could be widely available for routine clinical use.
authors.affiliation: Department of Nuclear Medicine and Molecular Imaging Center, Chang Gung Memorial Hospital, Taiwan, ROC.
authors.forename: Cheng-Hsiang
authors.initials: CH
authors.lastname: Yao
authors.forename: Kun-Ju
authors.initials: KJ
authors.lastname: Lin
authors.forename: Chi-Chang
authors.initials: CC
authors.lastname: Weng
authors.forename: Ing-Tsung
authors.initials: IT
authors.lastname: Hsiao
authors.forename: Yi-Shu
authors.initials: YS
authors.lastname: Ting
authors.forename: Tzu-Chen
authors.initials: TC
authors.lastname: Yen
authors.forename: Tong-Rong
authors.initials: TR
authors.lastname: Jan
authors.forename: Daniel
authors.initials: D
authors.lastname: Skovronsky
authors.forename: Mei-Ping
authors.initials: MP
authors.lastname: Kung
authors.forename: Shiaw-Pyng
authors.initials: SP
authors.lastname: Wey
mesh_terms: D000544:Alzheimer Disease / Q000000981:diagnostic imaging / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000378:metabolism*; D000814:Aniline Compounds; D001331:Automation; D002851:Chromatography, High Pressure Liquid; D005026:Ethylene Glycols; D005462:Fluorine Radioisotopes; D019983:Guideline Adherence; D006801:Humans; D049268:Positron-Emission Tomography
chemical_list: D016229:Amyloid beta-Peptides; D000814:Aniline Compounds; D005026:Ethylene Glycols; D005462:Fluorine Radioisotopes; C545186:florbetapir