Cited by 259Liver Disease Diagnosis and TreatmentDrug Transport and Resistance MechanismsLiver Diseases and Immunity

Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis

Adorini, Luciano, Pruzanski, Mark, Shapiro, David·2012·Drug Discovery Today

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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Crossref · 10.1016/j.drudis.2012.05.012

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Authors
Adorini, L., Pruzanski, M., & Shapiro, D.
Affiliations
Intercept Pharmaceuticals (United States) (US)
Corresponding author
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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