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Current Reviews in Clinical and Experimental Pharmacology


ISSN (Print): 2772-4328
ISSN (Online): 2772-4336

Mini-Review Article

A Short Review on Obeticholic Acid: An Effective Modulator of Farnesoid X Receptor

Author(s): Anila Kutty Narayanan*, Sudhindran Surendran, Dinesh Balakrishnan, Unnikrishnan Gopalakrishnan, Shweta Malick, Arun Valsan, Cyriac Abby Philips and Christopher John Edward Watson

Volume 19, Issue 3, 2024

Published on: 05 October, 2023

Page: [225 - 233] Pages: 9

DOI: 10.2174/0127724328239536230919070001

Price: $65


Farnesoid X receptor (FXR) was identified as an orphan nuclear receptor resembling the steroid receptor in the late ’90s. Activation of FXR is a crucial step in many physiological functions of the liver. A vital role of FXR is impacting the amount of bile acids in the hepatocytes, which it performs by reducing bile acid synthesis, stimulating the bile salt export pump, and inhibiting its enterohepatic circulation, thus protecting the hepatocytes against the toxic accumulation of bile acids. Furthermore, FXR mediates bile acid biotransformation in the intestine, liver regeneration, glucose hemostasis, and lipid metabolism. In this review, we first discuss the mechanisms of the disparate pleiotropic actions of FXR agonists. We then delve into the pharmacokinetics of Obeticholic acid (OCA), the first-in-class selective, potent FXR agonist. We additionally discuss the clinical journey of OCA in humans, its current evidence in various human diseases, and its plausible roles in the future.

Keywords: FXR, liver metabolism, bile acids, obeticholic acid, FXR agonist, pharmacokinetics.

Graphical Abstract
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