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Updated: Mar 26, 2026

Using Multi-fluorinated Bile Acids and In Vivo Magnetic Resonance Imaging to Measure Bile Acid Transport
Published on: November 27, 2016
Metabolic effects of bile acid sequestration: impact on cardiovascular risk factors
Valeria Spinelli1, Oscar Chávez-Talavera, Anne Tailleux
1aUniv Lille, UMR1011, EGID bInserm, UMR1011 cCHU Lille dInstitut Pasteur de Lille, U1011, Lille, France *Valeria Spinelli and Oscar Chávez-Talavera have contributed equally to the writing of this article.
Purpose Of Review:
This article discusses the impact of bile acid sequestrants (BAS) on cardiovascular risk factors (CVRFs), on the basis of recent (pre)clinical studies assessing the metabolic impact of modulation of enterohepatic bile acid signaling via the bile acid receptors farnesoid X receptor (FXR) and Takeda G-protein-coupled receptor 5 (TGR5).
Recent Findings:
BAS decrease low-density lipoprotein-cholesterol by stimulating de novo hepatic bile acid synthesis and lowering intestinal lipid absorption, and improve glucose homeostasis in type 2 diabetes mellitus, at least in part by increasing GLP-1 production, via intestinal TGR5- and FXR-dependent mechanisms. Intestinal and peripheral FXR and TGR5 modulation also affects peripheral tissues, which can contribute to the reduction of CVRFs.
Summary:
Bile acids are regulators of metabolism acting in an integrated interorgan manner via FXR and TGR5. Modulation of the bile acid pool size and composition, and selective interference with their receptors could, therefore, be a therapeutic approach to decrease CVRFs. Even though clinical cardiovascular outcome studies using BAS are still lacking, the existing data point to BAS as an efficacious pharmacological approach to reduce CVRFs.
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