ASB14780

ASB14780 is an orally active, small molecule inhibitor of cytosolic phospholipase A2 alpha (cPLA2α, also known as group IVA phospholipase A2). By targeting cPLA2α, the compound prevents the hydrolysis of membrane phospholipids into arachidonic acid, which is the rate-limiting step in the production of pro-inflammatory eicosanoids such as prostaglandins and leukotrienes. Developed by Asubio Pharma, ASB14780 has demonstrated high oral bioavailability and efficacy in preclinical models of nonalcoholic fatty liver disease (NAFLD), hepatic fibrosis, and asthma. Recent research also suggests that ASB14780 may have therapeutic potential in pancreatic cancers characterized by HDAC5 loss, which leads to the upregulation of cPLA2 and increased arachidonic acid metabolism, conferring sensitivity to cPLA2 inhibition.

Other names

3-[1-(4-phenoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoic acid 2-amino-2-(hydroxymethyl)propane-1,3-diol salt3-[1-(4-phenoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoic acid tris salt