Treatment of fibrosis using FXR ligands
AssigneeIntercept Pharmaceuticals, Inc.
InventorsStefano Fiorucci, Roberto Pellicciari, Mark Pruzanski
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Abstract
The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.
Claims19
A method for inhibiting fibrosis in a subject not suffering from a cholestatic condition, the method comprising the step of administering to the subject an effective amount of a ligand specific for the farnesoid X receptor (FXR), wherein the fibrosis to be inhibited occurs in an organ where FXR is expressed, with the proviso that the ligand is not chenodeoxyxholic acid (CDCA) or ursodeoxycholic acid (UDCA).
A method for inhibiting fibrosis in a subject not suffering from a cholestatic condition, the method comprising the step of administering to the subject an effective amount of a ligand specific for the farnesoid X receptor (FXR), wherein the fibrosis to be inhibited occurs in an organ where FXR is expressed, and wherein the ligand has an EC50 no greater than 5 μM in a cell-free FXR assay or in a cell-based FXR transactivation assay.
A kit for inhibiting fibrosis in a subject not suffering from a cholestatic condition, wherein the fibrosis to be inhibited occurs in an organ where farnesoid X receptor (FXR) is expressed, the kit comprising:
- an effective amount of a ligand specific for FXR, with the proviso that the ligand is not chenodeoxyxholic acid (CDCA) or ursodeoxycholic acid (UDCA);
- and,
- an instructional material teaching the indications, dosage, and schedule of administration of the ligand to the patient.
A kit for inhibiting fibrosis in a subject not suffering from a cholestatic condition, wherein the fibrosis to be inhibited occurs in an organ where farnesoid X receptor (FXR) is expressed, the kit comprising:
- an effective amount of a ligand specific for FXR, wherein the ligand has an EC50 no greater than 5 μM in a cell-free FXR assay or in a cell-based FXR transactivation assay;
- and,
- an instructional material teaching the indications, dosage, and schedule of administration of the ligand to the patient.
Dependencies are inferred from the claim text.