Flutafuranol (18F): A Comprehensive Review of a Promising Amyloid-β PET Imaging Agent for Alzheimer's Disease

1. Introduction to Flutafuranol (18F)

Overview

Flutafuranol (18F) is an investigational diagnostic radiopharmaceutical agent designed for use in positron emission tomography (PET) imaging. It is a fluorine-18 (18F) labeled molecular probe specifically developed for the in vivo visualization and quantification of amyloid-β (Aβ) plaques in the human brain.[1] The accumulation of Aβ plaques is a primary neuropathological hallmark of Alzheimer's disease (AD), a progressive neurodegenerative disorder and the most common cause of dementia.[1]

The ability to accurately detect and measure Aβ plaque burden in vivo is of paramount importance in the field of AD research and clinical practice. Amyloid PET imaging serves multiple critical roles: it aids in the early and differential diagnosis of AD from other forms of dementia, facilitates the stratification of patients for clinical trials targeting Aβ pathology, enables the monitoring of disease progression, and helps assess the pharmacodynamic effects of anti-amyloid therapeutic interventions.[3]

Rationale for Development

The development of flutafuranol (18F) was driven by the need to overcome certain limitations associated with earlier amyloid PET tracers. The pioneering amyloid PET tracer, 11C-Pittsburgh Compound B (11C-PiB), while demonstrating excellent imaging properties, is limited by the short 20-minute physical half-life of carbon-11. This necessitates an on-site cyclotron for its production, restricting its widespread clinical and research applicability.[19]