Abstract
Florbetaben is a fluorine-18 ((18)F)-labeled stilbene derivative that was developed as a positron emission tomography (PET) tracer for routine clinical application to visualize β-amyloid plaques in the Alzheimer's disease (AD) brain. The tracer successfully completed a global multicenter phase 0-III development program and was, as a consequence, recently approved by the US Food and Drug Administration and the European Medicines Agency. This review provides an overview on the florbetaben tracer characteristics and preclinical data leading to its human testing. Further, the favorable results of human pharmacokinetics, safety, and dosimetry evaluation of florbetaben are presented. Next, the results of the clinical testing of florbetaben are discussed, in which the tracer was shown to sensitively and specifically detect β-amyloid neuritic plaques, as evidenced by employing different gold standards (from clinical diagnosis to post mortem histopathology). The potential of florbetaben to predict AD dementia in cases of mild cognitive impairment and to assist in the differential diagnosis in cases of dementia is also described. Finally, potential clinical impact and clinical routine PET image acquisition and analysis protocols for florbetaben are discussed. Taken together, the evidence shows that florbetaben is a valuable β-amyloid-targeting PET tracer in the clinic with great potential to serve as a biomarker supporting clinical AD diagnosis.