Investigation of the Brain Biodistribution of the Lipoprotein-Associated Phospholipase A₂ (Lp-PLA₂) Inhibitor [¹⁸F]GSK2647544 in Healthy Male Subjects.

ABSTRACT:

Purpose

GSK2647544 is a potent and specific inhibitor of lipoprotein-associated phospholipase A₂ (Lp-PLA₂), which was in development as a potential treatment for Alzheimer's disease (AD). In order to refine therapeutic dose predictions and confirm brain penetration, a radiolabelled form of the inhibitor, [¹⁸F]GSK2647544, was manufactured for use in a positron emission tomography (PET) biodistribution study.

Procedures

[¹⁸F]GSK2647544 was produced using a novel, copper iodide (Cu(I)) mediated, [¹⁸F]trifluoromethylation methodology. Healthy male subjects (n = 4, age range 34-42) received an oral dose of unlabelled GSK2647544 (100 mg) and after 2 h an intravenous (iv) injection of [¹⁸F]GSK2647544 (average injecte

SUBMITTER: Huiban M 

PROVIDER: S-EPMC5209404 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature