turofexorate isopropyl (FXR-450) / Pfizer - LARVOL DELTA

SMRT regulation of nuclear receptors orchestrates bile acid homeostasis. (PubMed, Exp Mol Med) - "Treatment with a synthetic FXR agonist (XL335) rescued SMRTmRID1 mice during acute colitis. Collectively, these studies highlight the importance of SMRT in maintaining BA homeostasis through direct and indirect regulation of hepatic CAR and intestinal FXR activity, respectively, and point to potential therapeutic routes for combating intestinal pathologies associated with a high-fat diet."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammatory Bowel Disease • Oncology

Pharmacological characterization of second generation FXR agonists as effective EphA2 antagonists: a successful application of target hopping approach. (PubMed, Biochem Pharmacol) - "Herein we characterize new commercially available FXR (Farnesoid X Receptor) agonists as potential Eph ligands including Cilofexor, Nidufexor, Tropifexor, Turofexorate isopropyl and Vonafexor. Furthermore, Cilofexor interferes with the phosphorylation of EphA2 and the cell retraction and rounding in PC3 prostate cancer cells, both events depending on EphA2 activation. In conclusion, we can confirm that target hopping can be a successful approach to discover new moiety of protein-protein inhibitors."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

In Vitro Hepatic Steatosis Model based on Gut-liver-on-a-chip. (PubMed, Biotechnol Prog) - "The anti-steatotic effect of turofexorate isopropyl (XL-335) and metformin was tested, and both drugs showed different action mechanisms. In addition, the oxidative stress induced by lipid absorption was evaluated. Our results demonstrate the potential of the gut-liver chip for use as a novel, physiologically realistic in vitro model to study fatty liver disease."

Journal • Preclinical • Gastrointestinal Disorder • Hepatology