Species-dependent aromatase imaging in rodents, blood–brain barrier permeability, and tumor visualization with a novel 18F-labeled PET tracer, [18F]AromataPET-1

Abstract

This study developed a novel ¹⁸F-labeled PET tracer, [¹⁸F]AromataPET-1, based on the aromatase inhibitor [¹⁸F]BIBD-071, with the core goal of achieving specific in vivo imaging of aromatase in both the central nervous system and peripheral tissues, providing a tool for related disease research and clinical diagnosis. [¹⁸F]AromataPET-1 demonstrated high affinity, specific uptake in aromatase-rich tissues like the stomach and ovaries in rats, and excellent blood–brain barrier penetration, enabling brain imaging. It also showed specific tumor visualization in MCF-7 xenograft mouse models, whose uptake could be blocked by letrozole. Potential species-dependent differences in aromatase expression between mice and rats were suggested. [¹⁸F]AromataPET-1 is a promising tool for studying aromatase in peripheral tissues and for companion diagnostics in breast cancer.