Florbetapir (18F), a PET imaging agent that binds to amyloid plaques for the potential detection of Alzheimer's disease

Florbetapir (F-18), being developed by Avid Radiopharmaceuticals, is an F-18-labeled PET tracer binding to amyloid-beta (A beta) plaques for the potential detection of Alzheimer's disease (AD). Preclinical studies indicated high binding affinity of florbetapir (F-18) to A beta fibrils and specific labeling of A beta plaques in the cortical regions and hippocampus. In phase I and II clinical trials, florbetapir (F-18) clearly differentiated patients with AD from healthy controls and uptake was most prominent in the precuneus. The neocortical-to-cerebellar tracer uptake ratio reached a plateau within 50 min post-injection and high-quality images were acquired with 5 to 10 min image acquisition time with 370 MBq of florbetapir (F-18). Results from an ongoing phase III clinical trial confirmed a strong correlation between florbetapir (F-18) PET images and postmortem assessment of A beta deposition. No serious adverse events were reported in any of the clinical trials of florbetapir (F-18). At the time of publication, a marketing application for florbetapir (F-18) had been submitted to the US FDA. The fast kinetics and strong evidences of radiological-pathological correlation are advantages of florbetapir (F-18) over other F-18-labeled amyloid PET tracers. This tracer has a potential to serve as an agent for preclinical detection of AD-related pathology in the large elderly population.