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Mechanistic Modeling Revealed the Induction of Hepatic Transporters and Altered Bile Acid Disposition: Critical Factors in Drug Safety

BioIVT_ATQ2WBR_Bile Effects

FXR is a nuclear receptor that regulates genes involved in bile acid homeostasis. FXR agonists, such as obeticholic acid (OCA) and chenodeoxycholic acid, can increase mRNA and protein expression of some basolateral and canalicular efflux transporters.

Download the presentation to hear Dr. Cen Guo, from Pfizer, discuss:

  • Mechanistic modeling studies recently published in the Journal of Pharmacology and Experimental Therapeutics May 2018, “FXR Agonists Obeticholic Acid and Chenodeoxycholic Acid Increase Bile Acid Efflux in Sandwich-Cultured Human Hepatocytes: Functional Evidence and Mechanisms”*.
  • The compensatory mechanisms of hepatocytes after exposure to high concentrations of bile acids.
  • Direct functional evidence for the induction of bile acid efflux transporters by FXR agonists. 

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