Pharmaceutical compositions for combination therapy

Patent metadata

Field	Value
Publication number	US-11311557-B2
Application number	US-201615548537-A
Country	US
Kind code	B2
Filing date	Feb 5, 2016
Priority date	Feb 6, 2015
Publication date	Apr 26, 2022
Grant date	Apr 26, 2022

Abstract

The present invention relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one lipid lowering agent (e.g., PPAR-alpha agonist, PPAR-delta agonist, PPAR-alpha and delta dual agonist, and/or statin). Also disclosed is use of the combination for the treatment or prevention of a FXR mediated disease or condition, such as primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), portal hypertension, bile acid diarrhea, NAFLD (nonalcoholic fatty liver disease), NASH (non-alcohol-induced steatohepatitis), and other chronic liver diseases. The combination of the present invention is useful for the treatment or prevention of conditions related to elevated lipid and liver enzyme levels. The present invention also relates to packs or kits including the pharmaceutical combination.

First claim

The invention claimed is:

1. A pharmaceutical composition comprising:
a two-way combination of an FXR agonist and bezafibrate; and optionally one or more pharmaceutically acceptable carriers,
wherein the FXR agonist is a compound of formula (1):

or a pharmaceutically acceptable salt or amino acid conjugate thereof, and
wherein the pharmaceutical composition does not comprise any therapeutic agent other than the FXR agonist and bezafibrate,
wherein bezafibrate is in an amount of 80-400 mg, and
wherein the FXR agonist is in an amount of 1-30 mg.

2. The pharmaceutical composition of claim 1 , wherein bezafibrate is in an amount of 100-300 mg.

3. The pharmaceutical composition of claim 2 , wherein bezafibrate is in an amount of 100 mg.

4. The pharmaceutical composition of claim 2 , wherein bezafibrate is in an amount of 200 mg.

5. The pharmaceutical composition of claim 1 , wherein bezafibrate is in an amount of 400 mg.

6. The pharmaceutical composition of claim 1 , wherein the FXR agonist is in an amount of 5-25 mg.

7. The pharmaceutical composition of claim 1 , wherein bezafibrate is in the sustained release form.

8. The pharmaceutical composition of claim 7 , wherein bezafibrate is in an amount of 100-300 mg.

9. The pharmaceutical composition of claim 7 , wherein the FXR agonist is in an amount of 5-25 mg and bezafibrate is in an amount of 100-300 mg.

10. The pharmaceutical composition of claim 7 , wherein the FXR agonist is in an amount of 4-26 mg and bezafibrate is in an amount of 100-300 mg.

11. The pharmaceutical composition of claim 7 , wherein the composition is a unit dosage form.

12. The pharmaceutical composition of claim 11 , wherein the unit dosage form is a tablet or capsule.

13. The pharmaceutical composition of claim 1 , wherein the FXR agonist is in an amount of 5-25 mg and bezafibrate is in an amount of 100-300 mg.

14. The pharmaceutical composition of claim 1 , wherein the FXR agonist is in an amount of 4-26 mg and bezafibrate is in an amount of 100-300 mg.

15. The pharmaceutical composition of claim 1 , wherein the composition is a unit dosage form.

16. The pharmaceutical composition of claim 15 , wherein the unit dosage form is a tablet or capsule.

Assignees

• Intercept Pharmaceuticals Inc

Inventors

• Pruzanski Mark
• Adorini Luciano

Classifications

• A61K31/192

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• A61K31/40

  having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P1/16

  for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title