lanifibranor

Description: Lanifibranor (formerly named as IVA-337) is a novel, potent and well balanced agonist of the pan-peroxisome proliferator-activated receptors (PPAR) with excellent safety profiles and with EC50s of 1.5, 0.87 and 0.21 uM for human PPARalpha, PPARsigma and PPARgamma, respectively. Lanifibranor displayed strong activity in in vitro and in vivo models that are relevant to Non-Alcoholic Steato Hepatitis (NASH) pathophysiology suggesting the therapeutical potential for NASH patients. Lanifibranor demonstrated excellent anti-hyperglycemic and hypolipidemic efficacy in the db/db mouse model, and a significant anti-fibrotic activity in the mouse CCl4-induced liver fibrosis model. Contrasting with other PPARgamma agonists, Lanifibranor had no effect on hematocrit, plasma volume or heart weight in rats, which suggest that lanifibranor has the potential to be developed as therapeutics for the treatment of NASH.

References: J Med Chem. 2018 Mar 22; 61(6):2246-2265; Ann Rheum Dis. 2016 Dec; 75(12):2175-2183.