Tropifexor is an investigational drug that acts as an

agonist An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an R ...

of the

farnesoid X receptor The bile acid receptor (BAR), also known as farnesoid X receptor (FXR) or NR1H4 (nuclear receptor subfamily 1, group H, member 4), is a nuclear receptor that is encoded by the ''NR1H4'' gene in humans. Function FXR is expressed at high level ...

(FXR). It was discovered by researchers from

Novartis Novartis AG is a Swiss multinational corporation, multinational pharmaceutical company, pharmaceutical corporation based in Basel, Switzerland. Novartis is one of the largest pharmaceutical companies in the world and was the eighth largest by re ...

and

Genomics Institute of the Novartis Research Foundation Novartis AG is a Swiss multinational pharmaceutical corporation based in Basel, Switzerland. Novartis is one of the largest pharmaceutical companies in the world and was the eighth largest by revenue in 2024. Novartis manufactures the drugs c ...

. Its synthesis and pharmacological properties were published in 2017. It was developed for the treatment of cholestatic liver diseases and nonalcoholic steatohepatitis (NASH). In combination with cenicriviroc, a

CCR2 C-C chemokine receptor type 2 (CCR2 or CD192 (cluster of differentiation 192) is a protein that in humans is encoded by the ''CCR2'' gene. CCR2 is a CC chemokine receptor. Gene This CCR2 gene is located in the chemokine receptor gene cluste ...

and

CCR5 C-C chemokine receptor type 5, also known as CCR5 or CD195, is a protein on the surface of white blood cells that is involved in the immune system as it acts as a receptor for chemokines. In humans, the ''CCR5'' gene that encodes the CCR5 p ...

receptor inhibitor, it is undergoing a

phase II clinical trial The phases of clinical research are the stages in which scientists conduct experiments with a health intervention to obtain sufficient evidence for a process considered effective as a medical treatment. For drug development, the clinical phases ...

for NASH and

liver fibrosis Cirrhosis, also known as liver cirrhosis or hepatic cirrhosis, chronic liver failure or chronic hepatic failure and end-stage liver disease, is a chronic condition of the liver in which the normal functioning tissue, or parenchyma, is replaced ...

. 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 ] Half maximal effective concentration (EC50) is a measure of the concentration of a drug, antibody or toxicant which induces a stimulus–response model, biological response halfway between the baseline and maximum after a specified exposure tim ...

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.. Retrieved 17 May 2019.

References

{{FXR and LXR modulators Drugs developed by Novartis Benzothiazoles Farnesoid X receptor agonists Isoxazoles Tropanes Carboxylic acids Trifluoromethyl ethers Cyclopropyl compounds