BioCentury
ARTICLE | Distillery Therapeutics

Therapeutics: Lipoprotein-associated phospholipase A2 (PLA2G7; PAFAH; Lp-PLA2)

March 10, 2016 8:00 AM UTC

In vitro and rat studies identified a PLA2G7 inhibitor that could help treat DME. Chemical synthesis and in vitro studies of pyrimidone analogs identified a compound that inhibited PLA2G7 activity with an IC50 of 2.2 nM. In a rat model of DME, the compound decreased retinal thickness - a measure of disease severity - with potency comparable to the PLA2G7 inhibitor darapladib. In rats, the compound decreased PLA2G7 activity in serum compared with darapladib and had a plasma clearance rate of 18.6 mL/min/kg. Next steps could include further in vivo studies of the compound in DME and other progressive opthalmic diseases.

GlaxoSmithKline pls has darapladib (SB-480848; 480848) in Phase III testing to treat acute coronary syndrome (ACS), atherosclerosis and coronary artery disease (CAD) and Phase II testing to treat DME and Alzheimer's disease (AD)...