Tropifexor

Description: Tropifexor (also known as LJN452) is a novel, potent and highly potent agonist of FXR (farnesoid X receptor) with an EC50 value of 0.2 nM in HTRF assay. It shows potent in vivo activity in rodent PD models by measuring the induction of FXR target genes in various tissues. It has the potential for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH). Tropifexor has advanced into phase 2 human clinical trials in patients with NASH and PBC. The farnesoid X receptor (FXR) is a nuclear receptor that acts as a master regulator of bile acid metabolism and signaling. Activation of FXR inhibits bile acid synthesis and increases bile acid conjugation, transport, and excretion, thereby protecting the liver from the harmful effects of bile accumulation, leading to considerable interest in FXR as a therapeutic target for the treatment of cholestasis and nonalcoholic steatohepatitis.

References: J Med Chem. 2017 Dec 28; 60(24):9960-9973; Therap Adv Gastroenterol. 2017 Oct; 10(10): 791–803; Hepatology. 2017 Apr; 65(4):1393-1404.