Tropifexor

Tropifexor

Tropifexor

Chemical compound

Tropifexor is an investigational drug that acts as an agonist of the farnesoid X receptor (FXR). It was discovered by researchers from Novartis and Genomics Institute of the Novartis Research Foundation. Its synthesis and pharmacological properties were published in 2017.[1] It was developed for the treatment of cholestatic liver diseases and nonalcoholic steatohepatitis (NASH). In combination with cenicriviroc, a CCR2 and CCR5 receptor inhibitor, it is undergoing a phase II clinical trial for NASH and liver fibrosis.[2]

Quick Facts Clinical data, ATC code ...

Rats treated orally with tropifexor (0.03 to 1 mg/kg) showed an upregulation of the FXR target genes, BSEP and SHP, and a down-regulation of CYP8B1. Its EC50 for FXR is between 0.2 and 0.26 nM depending on the biochemical assay.

The patent that covers tropifexor and related compounds was published in 2010.[3]

References

  1. [1]
    Tully DC, Rucker PV, Chianelli D, Williams J, Vidal A, Alper PB, et al. (December 2017). "Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH)". Journal of Medicinal Chemistry. 60 (24): 9960–9973. doi:10.1021/acs.jmedchem.7b00907. PMID 29148806.
  2. [2]
    Clinical trial number NCT03517540 for "Safety, Tolerability, and Efficacy of a Combination Treatment of Tropifexor (LJN452) and Cenicriviroc (CVC) in Adult Patients With Nonalcoholic Steatohepatitis (NASH) and Liver Fibrosis. (TANDEM)" at ClinicalTrials.gov
  3. [3]
    WO Application Filing 2012087519, Alper PB, Chianelli D, Mutnick D, Vincent P, Tully DC, "Compositions and methods for modulating fxr", published 2012-06-28, assigned to Genomics Institute of the Novartis Research Foundation. Retrieved 17 May 2019.


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