[18F]F-diarylbisthiazole

[18F]F-diarylbisthiazole refers to a class of fluorine-18 labeled diarylbisthiazole (DABTA) derivatives developed as positron emission tomography (PET) imaging tracers for the non-invasive detection of alpha-synuclein (α-syn) aggregates in the brain. These tracers are designed to address the critical unmet medical need for specific biomarkers to diagnose and monitor alpha-synucleinopathies, including Parkinson's disease, dementia with Lewy bodies (DLB), and multiple system atrophy (MSA). Developed through a collaborative academic effort involving the Philipps University of Marburg, Technical University of Munich, Karolinska Institutet, Uppsala University, and Ludwig-Maximilians-University of Munich, these compounds utilize a diarylbisthiazole scaffold. The incorporation of a methylenedioxy group significantly enhances binding affinity to α-syn fibrils (with subnanomolar to low nanomolar Ki values) and provides high selectivity over beta-amyloid (Aβ) and tau fibrils. Preclinical evaluations of lead candidates, such as [18F]FS9, [18F]d6, and [18F]d8, have demonstrated favorable brain uptake, rapid washout kinetics, and high metabolic stability in animal models, as well as specific binding in postmortem human brain tissues.

Other names

18F-labeled diarylbisthiazoles18F-labeled disarylbisthiazoles[18F]F-diarylbisthiazolesdiarylbisthiazole-based PET tracers