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Updated: Jun 12, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
10:51

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Published on: November 15, 2013

Farnesoid X receptor modulators: a patent review

Matthew Lantz Crawley1

  • 1Origin Pharmaceuticals, Inc., Wayne, PA 19087, USA. mlcrawley@originpharmaceuticals.com

Expert Opinion on Therapeutic Patents
|June 24, 2010
PubMed
Abstract

Insights

New farnesoid X receptor (FXR) agonists show promise for treating dyslipidemia. These compounds are effective and safe in preclinical studies, offering potential new therapies for cholesterol management and other conditions.

Area of Science:

  • Pharmacology
  • Biochemistry
  • Drug Discovery

Background:

  • Farnesoid X receptor (FXR) regulates cholesterol, triglyceride, and lipogenesis pathways.
  • Dyslipidemia treatment requires novel medications due to statin intolerance.
  • FXR agonists represent a promising therapeutic avenue for metabolic disorders.

Purpose of the Study:

  • To review recent advances in novel FXR modulators.
  • To focus on patent applications and publications from the last five years.

Main Methods:

  • Systematic review of 72 patent applications and peer-reviewed articles.
  • Analysis of 16 generic structure classes and nearly 5000 synthesized structures.
  • Survey of structure-activity relationships, in vitro, and in vivo efficacy.

Main Results:

  • Identified 16 distinct structural classes of FXR modulators.
  • Nearly 5000 novel compounds were synthesized and analyzed.
  • Revealed insights into structure-activity relationships and therapeutic potential.

Conclusions:

  • FXR agonists demonstrate efficacy and safety in primate models.
  • Significant potential exists for treating dyslipidemia.
  • Potential applications extend to other disease areas beyond metabolic disorders.

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