In vivo quantification of [¹¹C]BIO-1819578 in non-human primates, a novel radioligand for O-GlcNAcase.

ABSTRACT: Neurofibrillary tangles (NFTs), composed of aggregated tau protein, in the brain is a neuropathological hallmark and feature of Alzheimer's disease (AD) and other tauopathies. One promising approach to prevent tau aggregates is to inhibit O-GlcNAcase (OGA), an enzyme that regulates tau O-GlcNAcylation. [¹¹C]BIO-1819578 has emerged as a promising candidate to determine target occupancy of such OGA inhibitor drugs. The aim of this study was to further evaluate the pharmacokinetic properties of [¹¹C]BIO-1819578 in non-human primates (NHPs) and to estimate its effective dose. Kinetic compartment analyses of [¹¹C]BIO-1819578 binding to OGA in the brain were performed on positron emission tomography (PET) measurements conducted in three cynomolgus NHPs. Whole-bod

SUBMITTER: Bolin M 

PROVIDER: S-EPMC11994644 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature