Formulations of dazucorilant, a glucocorticoid receptor modulator

Patent metadata

Field	Value
Publication number	US-12370188-B2
Application number	US-202318481549-A
Country	US
Kind code	B2
Filing date	Oct 5, 2023
Priority date	Oct 6, 2022
Publication date	Jul 29, 2025
Grant date	Jul 29, 2025

Abstract

The present invention provides formulations of (R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(pyridin-2-yl)methanone, and methods of making and using the same.

First claim

What is claimed is:

1. A unit dosage form for oral administration, wherein the unit dosage form comprises a hard gelatin capsule containing a composition, the composition comprising:
Compound I, (R)-(1-(4-fluorophenyl)-6-((4-(trifluoromethyl)phenyl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(pyridin-2-yl)methanone:

in an amount of about 18.75% (w/w);

polyethylene glycol having a molecular weight of about 400 Daltons (PEG400), in an amount of about 6.5% (w/w); and
Vitamin E polyethylene glycol succinate (Vitamin E TPGS), in an amount of about 74.75% (w/w).

2. The unit dosage form of claim 1 , wherein Compound I is present in an amount of from about 50 mg to about 150 mg.

3. The unit dosage form of claim 1 , wherein the composition comprises:
Compound I, in an amount of about 50 mg;
PEG400, in an amount of about 17 mg; and
Vitamin E TPGS, in an amount of about 199 mg.

4. The unit dosage form of claim 1 , wherein the composition comprises:
Compound I, in an amount of about 75 mg;
PEG400, in an amount of about 26 mg; and
Vitamin E TPGS, in an amount of about 299 mg.

5. The unit dosage form of claim 1 , wherein the composition comprises:
Compound I, in an amount of about 100 mg;
PEG400, in an amount of about 35 mg; and
Vitamin E TPGS, in an amount of about 399 mg.

6. The unit dosage form of claim 1 , wherein the composition comprises:
Compound I, in an amount of about 150 mg;
PEG400, in an amount of about 52 mg; and
Vitamin E TPGS, in an amount of about 598 mg.

7. The unit dosage form of claim 1 , wherein the composition consists essentially of:
Compound I, in an amount of 50 mg;
PEG400, in an amount of 17 mg; and
Vitamin E TPGS, in an amount of 199 mg.

8. The unit dosage form of claim 1 , wherein the composition consists essentially of:
Compound I, in an amount of 75 mg;
PEG400 in an amount of 26 mg; and
Vitamin E TPGS in an amount of 299 mg.

9. The unit dosage form of claim 1 , wherein the composition consists essentially of:
Compound I, in an amount of 100 mg;
PEG400, in an amount of 35 mg; and
Vitamin E TPGS, in an amount of 399 mg.

10. The unit dosage form of claim 1 , wherein the composition consists essentially of:
Compound I, in an amount of 150 mg;
PEG400, in an amount of 52 mg; and
359, Vitamin E TPGS, in an amount of 598 mg.

Assignees

• Corcept Therapeutics Inc

Inventors

• Bastin Rick
• Hosny Alla
• Jacob Dolly
• Lin Wu

Classifications

• A61K47/22

  Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones · CPC title

• A61K9/4858

  Organic compounds · CPC title

• A61K9/4825

  Proteins, e.g. gelatin (gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816) · CPC title

• A61K9/4866 Primary

  Organic macromolecular compounds · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title