Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis
Abstract
Nonalcoholic fatty liver disease (NAFLD) is a highly prevalent chronic liver condition evolving in a proportion of patients into nonalcoholic steatohepatitis (NASH), an aggressive form of NAFLD associated with increased cardiovascular mortality and significant risk of progressive liver disease, including fibrosis, cirrhosis and hepatocellular carcinoma. At present, no specific therapies for NASH exist. In this review, we examine the evidence supporting activation of the farnesoid X receptor (FXR), a nuclear hormone receptor regulated by bile acids (BAs), for the treatment of NASH. We also discuss the potential of the semi-synthetic BA derivative obeticholic acid (OCA), a first-in-class FXR agonist, as a safe and effective drug to address this significant unmet medical need.
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FXR also modulates immune response and inflammation.
“In addition to mediating the anticholestatic and antifibrotic effects of obeticholic acid, FXR also modulates immune response and inflammation. 26”
From A Placebo-Controlled Trial of Obeticholic Acid in Primary Biliary Cholangitis (2016) · cites this paper as [26]
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Self-citation
- Authors
- Adorini, L., Pruzanski, M., & Shapiro, D.
- Affiliations
- Intercept Pharmaceuticals (United States) (US)
- Corresponding author
- Adorini, Luciano
- ORCID
- Adorini, Luciano
- Venue
- Drug Discovery Today
- Publisher
- Elsevier BV
- Published
- 2012-09
- Volume
- 17
- Issue
- 17-18
- Pages
- 988-997
- ISSN
- 1359-6446 (ISSN-L)
- OpenAlex
- W2052064885
- Cited by
- 259
- References
- 13
- Citations by year
- 2026: 4 · 2025: 7 · 2024: 10 · 2023: 12 · 2022: 12 · 2021: 25 · 2020: 17 · 2019: 10 · 2018: 30 · 2017: 27 · 2016: 26 · 2015: 19 · 2014: 34 · 2013: 24 · 2012: 2
- FWCI
- 3.19
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drug Discovery Today (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Epidemiology › Liver Disease Diagnosis and Treatment
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Health Sciences › Medicine › Hepatology › Liver Diseases and Immunity
- Keywords
- farnesoid X receptor, nonalcoholic steatohepatitis, non-alcoholic fatty liver disease, bile acids, obeticholic acid, FXR agonists, nuclear receptors, NASH therapy, liver fibrosis
- MeSH terms
- Receptor, Farnesoid X-Activated, Animals, Chenodeoxycholic Acid, Fatty Liver, Humans, Receptors, Cytoplasmic and Nuclear, Non-alcoholic Fatty Liver Disease
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