Evidence map›Paper›PMID 29226620›Full record

ArticlePharmacology research & perspectives2017

Comparative potency of obeticholic acid and natural bile acids on FXR in hepatic and intestinal in vitro cell models.

Yuanyuan Zhang, Carl LaCerte, Sanjay Kansra, Jonathan P Jackson, Kenneth R Brouwer, Jeffrey E Edwards

Open access · goldAbstract readComparative Study
In one paragraph

Article in Pharmacology research & perspectives, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed
1.6field-weighted citation impact, top 14% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

22 citing papers in PubMed, 33 citations in OpenAlex.

  1. Trial
  2. Trial
  3. Review
  4. Article
  5. Article
  6. Article
  7. Bile acids as therapeutic agents.Frontiers in pharmacology · 2025
    Review
  8. Article
  9. Review
  10. Impact of Primary and Secondary Bile Acids onPolish journal of microbiology · 2022
    Review
  11. Article
  12. Sex differences feed into nuclear receptor signaling along the digestive tract.Biochimica et biophysica acta. Molecular basis of disease · 2021
    Review
  13. Review
  14. Article
  15. Review
  16. Chronic diarrhea, bile acids, and Clostridia.The Journal of clinical investigation · 2020
    Article
  17. Review
  18. Review
  19. Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

6 authors at 2 institutions in 2 countries.

Yuanyuan ZhangIntercept Pharmaceuticals Inc., San Diego, CA, USA.
Carl LaCerteIntercept Pharmaceuticals Inc., San Diego, CA, USA.
Sanjay KansraIntercept Pharmaceuticals Inc., San Diego, CA, USA.
Jonathan P JacksonQualyst Transporter Solutions, LLC, Durham, NC, USA.
Kenneth R BrouwerQualyst Transporter Solutions, LLC, Durham, NC, USA.
Jeffrey E EdwardsIntercept Pharmaceuticals Inc., San Diego, CA, USA.ORCID 0000-0003-2732-8201
Intercept Pharmaceuticals (United States) · USNational Transport University · UA

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Obeticholic acid (OCA) is a semisynthetic farnesoid X receptor (FXR) agonist, an analogue of chenodeoxycholic acid (CDCA) which is indicated for the treatment of primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA). OCA efficiently inhibits bile acid synthesis and promotes bile acid efflux via activating FXR-mediated mechanisms in a physiologically relevant in vitro cell system, Sandwich-cultured Transporter Certified ™ human primary hepatocytes (SCHH). The study herein evaluated the effects of UDCA alone or in combination with OCA in SCHH. UDCA (≤100 μmol/L) alone did not inhibit CYP7A1 mRNA, and thus, no reduction in the endogenous bile acid pool observed. UDCA ≤100 μmol/L concomitantly administered with 0.1 μmol/L OCA had no effect on bile acid synthesis beyond what was observed with OCA alone. Furthermore, this study evaluated human Caco-2 cells (clone C2BBe1) as in vitro intestinal models. Glycine conjugate of OCA increased mRNA levels of FXR target genes in Caco-2 cells, FGF-19, SHP, OSTα/β, and IBABP, but not ASBT, in a concentration-dependent manner, while glycine conjugate of UDCA had no effect on the expression of these genes. The results suggested that UDCA ≤100 μmol/L did not activate FXR in human primary hepatocytes or intestinal cell line Caco-2. Thus, co-administration of UDCA with OCA did not affect OCA-dependent pharmacological effects.

Indexed as

AnimalsBile Acids and SaltsCaco-2 CellsCells, CulturedChenodeoxycholic AcidCholesterol 7-alpha-HydroxylaseGene Expression RegulationHumansIntestinal MucosaIntestinesIn Vitro TechniquesLiverModels, BiologicalReceptor, Farnesoid X-ActivatedReceptors, Cytoplasmic and NuclearBile Acids and SaltsChenodeoxycholic AcidCholesterol 7-alpha-HydroxylaseCYP7A1 protein, humanobeticholic acidReceptor, Farnesoid X-ActivatedReceptors, Cytoplasmic and Nuclearbile acidscaco-2 cellsFXRhepatocytesobeticholic acidursodeoxycholic acid

Identifiers

PMID29226620
PMCPMC5723701
OpenAlexW2765410098

What OpenQuestion holds

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LicenceCC BY-NC-ND
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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.