Synonyms: example 13/9 [US10485795B2] | GS-9674 | GS9674
Compound class:
Synthetic organic
Comment: Cilofexor (GS-9674) is a nonsteroidal farnesoid X receptor (FXR) agonist. It was originally identified by Phenex Pharmaceuticals [2] and is being developed by Gilead Pharmaceuticals for hepatic anti-steatotic activity, and potential to treat nonalcoholic fatty liver disease (NAFLD) and/or nonalcoholic steatohepatitis (NASH) [1,4]. Successful treatment of these liver conditions will most likely be achieved using combinations of antilipemic, anti-inflammatory and anti-fibrotic agents.
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Hollenback D, Hambruch E, Fink G, Birkel M, Schulz A, Hornberger M, Liu K, Staiger KM, Krol HD, Deuschle U et al.. (2024)
Development of Cilofexor, an intestinally-biased Farnesoid X Receptor agonist, for the treatment of fatty liver disease. J Pharmacol Exp Ther, [Epub ahead of print]. [PMID:38409114] |
2. Kinzel O, Steeneck C, Kremoser C. (2013)
Novel fxr (nr1h4) binding and activity modulating compounds. Patent number: WO2013007387. Assignee: Phenex Pharmaceuticals. Priority date: 13/07/2011. Publication date: 17/01/2013. |
3. Kinzel O, Steeneck C, Kremoser C. (2019)
FXR (NR1H4) binding and activity modulating compounds. Patent number: US10485795B2. Assignee: Gilead Sciences Inc. Priority date: 13/07/2011. Publication date: 26/11/2019. |
4. Romero FA, Jones CT, Xu Y, Fenaux M, Halcomb RL. (2020)
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease. J Med Chem, 63 (10): 5031-5073. [PMID:31930920] |
5. Trauner M, Gulamhusein A, Hameed B, Caldwell S, Shiffman ML, Landis C, Eksteen B, Agarwal K, Muir A, Rushbrook S et al.. (2019)
The Nonsteroidal Farnesoid X Receptor Agonist Cilofexor (GS-9674) Improves Markers of Cholestasis and Liver Injury in Patients With Primary Sclerosing Cholangitis. Hepatology, 70 (3): 788-801. [PMID:30661255] |