Lanifibranor

Lanifibranor is an agonist of peroxisome proliferator-activated receptors (PPARs) with EC₅₀ values of 1,537, 866, and 206 nM for human recombinant PPARα, PPARβ, and PPARγ, respectively, for transactivation activity.¹ It increases β-oxidation in Huh-7 and C2C12 cells when used at concentrations of 1 and 3 µM, respectively, and increases the expression of the PPARγ target genes adipocyte protein 2 (aP2) and adiponectin in adipocytes. Lanifibranor reduces plasma glucose and triglyceride levels in a db/db mouse model of type 2 diabetes when administered at doses of 10 and 30 mg/kg for five days. It also increases plasma adiponectin levels and decreases collagen deposition in a carbon tetrachloride-induced mouse model of non-alcoholic steatohepatitis (NASH).

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1. Boubia, B., Poupardin, O., Barth, M., et al. Design, synthesis, and evaluation of a novel series of indole sulfonamide peroxisome proliferator activated receptor (PPAR) α/γ/δ triple activators: Discovery of lanifibranor, a new antifibrotic clinical candidate. J. Med. Chem. 61(6), 2246-2265 (2018).