Granted Patent
B2
US 12,514,849 · App. 18/427,477 · Granted Jan 6, 2026
Pharmaceutical formulations containing relacorilant, a heteroaryl-ketone fused azadecalin compound
Assignee:
Corcept Therapeutics Incorporated
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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.
Claims (18)
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).
Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST
Recorded Feb 5, 2024
From: SCOTT, IAN; LEMONS, TRAVIS; CHIA, YIP-FONG
To: CORCEPT THERAPEUTICS INCORPORATED
Reel/Frame 066386/0932 →
Continuity (4)
Provisional Application
62781983
· Dec 19, 2018
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