REVIEW article
Front. Pharmacol.
Sec. Gastrointestinal and Hepatic Pharmacology
Bile Acids as Therapeutic Agents
Provisionally accepted
- 1Johns Hopkins University, Baltimore, United States
- 2Johns Hopkins Medicine, Baltimore, United States
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Bile acids (BAs) are amphiphilic molecules traditionally recognized for their role in lipid digestion but have gained increased interest for their therapeutic potential. Among them, ursodeoxycholic acid (UDCA) is the most widely prescribed and has been FDA-approved in the treatment of primary biliary cholangitis (PBC), the most common chronic cholestatic liver disease, while also being used off-label in multiple other disorders. The therapeutic effects of BAs are linked to their capacity to modulate signaling pathways, reduce hepatocellular injury, and regulate inflammation. Their physicochemical properties, particularly hydrophobicity, influence both efficacy and toxicity, of which the mechanisms involving receptors such as farnesoid X receptor (FXR), vitamin D receptor (VDR) and Takeda G protein-coupled receptor 5 (TGR5) help to explain. Recent regulatory milestones include the FDA-approval of chenodeoxycholic acid (CDCA) in the treatment of cerebrotendinous xanthomatosis (CTX) and ongoing clinical trials such as that of norucholic acid (NCA) in the treatment of primary sclerosing cholangitis (PSC). Expanding research is redefining the BA therapeutic landscape, with applications spanning cholestatic, metabolic, and neurodegenerative diseases. This review will explore established and emerging BA-based monotherapies, combination regimens, and novel BA-driven drug delivery systems.
Keywords: bile acid therapy, Bile acids, Bilosomes, Cholestasis, FXR, Neuroprotection, TGR5 activation, UDCA
Received: 26 Oct 2025; Accepted: 08 Dec 2025.
Copyright: © 2025 Vu, Kawamoto, Villalba-Davila, Dong and Karnsakul. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence: Wikrom Karnsakul
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