Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound

Patent metadata

Field	Value
Publication number	US-12514849-B2
Application number	US-202418427477-A
Country	US
Kind code	B2
Filing date	Jan 30, 2024
Priority date	Dec 19, 2018
Publication date	Jan 6, 2026
Grant date	Jan 6, 2026

Abstract

Disclosed herein are novel formulations containing relacorilant ((R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone) that are suitable for administration, including oral administration, to patients suffering from disorders amenable to treatment by glucocorticoid receptor modulators (GRMs). Single unit dosage forms comprise softgel capsules containing these formulations. Such softgel capsules may contain, e.g., relacorilant formulations containing 25 milligrams (mg), 50 mg, 100 mg, 200 mg, 300 mg, 400 mg, 500 mg, or other amounts of relacorilant. These novel formulations and single unit dosage forms may be used to treat diseases and disorders including Cushing's syndrome, Cushing's Disease, and other disorders.

First claim

We claim:

1 . A formulation for oral administration of relacorilant, (R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl) sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl) (4-(trifluoromethyl) pyridin-2-yl) methanone, which has the following structure:

the formulation comprising:
about 20% relacorilant;
about 60% polyoxyl glyceride compounds;
and
about 20% propylene glycol compounds, wherein said percentages are weight percent.

2 . The formulation of claim 1 , further including an antioxidant selected from butylated hydroxyanisole (BHA) and butylated hydroxytoluene (BHT).

3 . The formulation of claim 2 , wherein the formulation comprises about 0.02% antioxidant.

4 . The formulation of claim 2 , wherein the polyoxyl glyceride compounds are lauroyl polyoxy glyceride compounds.

5 . The formulation of claim 2 , consisting of 20% relacorilant, 59.98% Lauroyl poloxyl-32 glycerides, 20% Propylene glycol monocaprylate, and 0.02% Butylated hydroxytoluene (BHT).

6 . The formulation of claim 5 , consisting of 25 mg relacorilant, 74.975 mg Lauroyl poloxyl-32 glycerides, 25 mg Propylene glycol monocaprylate, and 0.025 mg Butylated hydroxytoluene (BHT).

7 . The formulation of claim 5 , consisting of 50 mg relacorilant, 149.95 mg Lauroyl poloxyl-32 glycerides, 50 mg Propylene glycol monocaprylate, and 0.05 mg Butylated hydroxytoluene (BHT).

8 . The formulation of claim 5 , consisting of 100 mg relacorilant, 299.9 mg Lauroyl poloxyl-32 glycerides, 100 mg Propylene glycol monocaprylate, and 0.1 mg Butylated hydroxytoluene (BHT).

9 . The formulation of claim 5 , consisting of 200 mg relacorilant, 599.8 mg Lauroyl poloxyl-32 glycerides, 200 mg Propylene glycol monocaprylate, and 0.2 mg Butylated hydroxytoluene (BHT).

10 . The formulation of claim 5 , consisting of 300 mg relacorilant, 899.7 mg Lauroyl poloxyl-32 glycerides, 300 mg Propylene glycol monocaprylate, and 0.3 mg Butylated hydroxytoluene (BHT).

11 . The formulation of claim 5 , consisting of 400 mg relacorilant, 1199.6 mg Lauroyl poloxyl-32 glycerides, 400 mg Propylene glycol monocaprylate, and 0.4 mg Butylated hydroxytoluene (BHT).

12 . The formulation of claim 5 , consisting of 500 mg relacorilant, 1499.5 mg Lauroyl poloxyl-32 glycerides, 500 mg Propylene glycol monocaprylate, and 0.5 mg Butylated hydroxytoluene (BHT).

13 . The formulation of claim 5 , consisting of 750 mg relacorilant, 2249.25 mg Lauroyl poloxyl-32 glycerides, 750 mg Propylene glycol monocaprylate, and 0.75 mg Butylated hydroxytoluene (BHT).

Assignees

• Corcept Therapeutics Inc

Inventors

• Scott Ian
• Lemons Travis
• Chia Yip-Fong

Classifications

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K9/4808

  characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084) · CPC title

• A61K9/4866

  Organic macromolecular compounds · CPC title

• A61K47/10

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