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Gluco-Metabolic Effects of Pharmacotherapy-Induced Modulation of Bile Acid Physiology

Andreas Brønden1, Filip K Knop1,2,3,4

  • 1Center for Clinical M etabolic Research, Gentofte Hospital, University of Copenhagen, DK-2900 Hellerup, Denmark.

The Journal of Clinical Endocrinology and Metabolism
|October 21, 2019
PubMed
Abstract

Insights

Bile acid receptors like FXR and TGR5 influence glucose metabolism. While FXR agonists show potential, TGR5 agonists have safety concerns, and other treatments modulate bile acids for glucose control.

Area of Science:

  • Endocrinology and Metabolism
  • Gastroenterology
  • Pharmacology

Background:

  • Bile acid receptors, farnesoid X receptor (FXR) and Takeda G protein-coupled receptor 5 (TGR5), are key regulators of glucose metabolism.
  • Modulation of these receptors impacts incretin secretion, insulin, glucagon, energy expenditure, and gut microbiota.

Purpose of the Study:

  • To review the link between bile acid physiology and glucose metabolism.
  • To focus on the gluco-metabolic effects of treatments targeting bile acid pathways.

Main Methods:

  • Literature search using keywords: FXR, TGR5, agonist, ASBT, bile acid sequestrant, metformin, glucose metabolism.
  • Manual searches of reference lists and conference proceedings.

Main Results:

  • FXR agonists' gluco-metabolic benefits require further evidence.
  • TGR5 agonists face safety concerns, limiting clinical relevance.
  • ASBT inhibitors, bile acid sequestrants, and metformin demonstrate glucose-lowering effects partly via bile acid modulation.

Conclusions:

  • Optimizing bile acid-modulating therapies is possible due to their role in glucose regulation.
  • Further research is needed to establish FXR agonist efficacy and address TGR5 agonist safety concerns.
Keywords:
ASBTFXRTGR5bile acid sequestrantmetformin

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