GMP-compliant automated synthesis of [18F]AV-45 (Florbetapir F 18) for imaging β-amyloid plaques in human brain

We report herein the Good Manufacturing Practice (GMP)-compliant automated synthesis of 18F-labeled styrylpyridine, AV-45 (Florbetapir), a novel tracer for positron emission tomography (PET) imaging of β-amyloid (Aβ) plaques in the brain of Alzheimer’s disease patients. [18F]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 [18F]AV-45 reached as high as 470±135 TBq/mmol (n=19). The present studies show that [18F]AV-45 can be manufactured under GMP-compliant conditions and could be widely available for routine clinical use.