PF-8380

PF-8380 is a potent, selective, and orally bioavailable small molecule inhibitor of autotaxin (ATX), an enzyme also known as ectonucleotide pyrophosphatase/phosphodiesterase 2 (ENPP2). ATX is responsible for the production of lysophosphatidic acid (LPA) from lysophosphatidylcholine (LPC). LPA is a bioactive lipid that signals through specific G protein-coupled receptors to promote cell proliferation, migration, and survival. PF-8380 effectively lowers LPA levels in vivo and has been utilized in preclinical research to investigate the role of the ATX-LPA axis in various pathologies, including inflammatory diseases like colitis, neuropathic pain, and various cancers such as breast cancer. It was originally developed by Pfizer as a pharmacological tool to validate ATX as a therapeutic target.

Other names

(3,5-dichlorophenyl)methyl 4-[3-oxo-3-(2-oxo-3H-1,3-benzoxazol-6-yl)propyl]piperazine-1-carboxylate