GSK2647544

GSK2647544 is a potent and selective small molecule inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme implicated in inflammatory processes and vascular disease. It was developed by GSK as a potential treatment for Alzheimer's disease, based on the hypothesis that Lp-PLA2 inhibition could reduce neuroinflammation associated with the condition. The drug demonstrated good oral bioavailability, dose-dependent inhibition of plasma Lp-PLA2 activity, and measurable brain penetration in healthy volunteers. However, development was discontinued after clinically significant drug-drug interactions were observed with simvastatin[1][6][3][4].