IP Library Granted Patent US 12,083,131
Granted Patent B2
US 12,083,131 · App. 16/786,160 · Granted Sep 10, 2024

Neuroactive steroids, compositions, and uses thereof

Inventors: Stephen Jay Kanes (Brynlawn, PA); Helen Colquhoun (Arlington, MA)
Assignee: Sage Therapeutics, Inc.
A61K31/573A61K9/0019A61K9/0053A61K31/57A61K47/40
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Quick Facts
Patent No.
US 12,083,131
App. No.
16/786,160
Granted
Sep 10, 2024
Kind
B2
Abstract

Described herein are methods of treating tremor, e.g., essential tremor, depression, e.g., postpostum depression; and anxiety disorder, the method comprising administering to a human subject suffering from tremor, e.g., essential tremor; depression, e.g., postpostum depression, an anxiety disorder with a neuroactive steroid or a composition comprising a neuroactive steroid (e.g., pregnanolone, allopregnanolone, alphadalone, ganaxolone, or alphaxolone).

Claims (25)

1. A method of treating postpartum depression in a human subject, the method comprising administering a continuous intravenous infusion of allopregnanolone, wherein the infusion comprises administering a first infusion, second infusion, and third infusion to the subject in need thereof, and wherein the first infusion delivers a smaller amount, as measured in μg/kg/hour, of allopregnanolone/unit time than the second infusion, and wherein the third infusion delivers a smaller amount, as measured in μg/kg/hour, of allopregnanolone/unit time than the second infusion, and wherein

said first infusion comprises administering a continuously increasing amount of allopregnanolone at an amount of allopregnanolone/unit time of 5-100 μg/kg/hour, 10-80 μg/kg/hour, or 15-70 μg/kg/hour;

said second infusion comprises administering an amount of allopregnanolone/unit time of 50-100 μg/kg/hour, 70-100 μg/kg/hour, or 86 μg/kg/hour; and

said third infusion comprises administering a continuously decreasing amount of allopregnanolone at an amount of allopregnanolone/unit time of 5-100 μg/kg/hour, 10-80 μg/kg/hour, or 15-70 μg/kg/hour.

2. The method of claim 1 , wherein the first infusion comprises administering a plurality of step doses, wherein each subsequent step dose delivers a larger amount of allopregnanolone/unit time than the step dose that precedes it.

3. The method of claim 1 , wherein the third infusion comprises administering a plurality of step doses, wherein each subsequent step dose delivers a smaller amount, as measured in μg/kg/hour, of allopregnanolone/unit time than the step dose that precedes it, wherein the plurality of step doses comprises a first, second, and third step dose.

4. The method of claim 1 , wherein the allopregnanolone is administered at a dose of 60-100 μg/kg/hour during the second infusion.

5. The method of claim 1 , wherein the allopregnanolone is administered at the same amount of allopregnanolone/unit time over the entire second infusion.

6. The method of claim 1 , wherein

said first infusion comprises administering a continuously increasing amount of allopregnanolone at an amount allopregnanolone/unit time of 15-70 μg/kg/hour;

said second infusion comprises administering an amount of allopregnanolone/unit time of 50-100 μg/kg/hour; and

said third infusion comprises administering a continuously decreasing amount of allopregnanolone at an amount of allopregnanolone/unit time of 15-70 μg/kg/hour.

7. The method of claim 1 , wherein

said first infusion comprises administering a plurality of step doses, wherein each subsequent step dose delivers a larger amount of allopregnanolone/unit time than the step dose that precedes it, and the amount of allopregnanolone/unit time administered is 5-100 μg/kg/hour, 10-80 μg/kg/hour, or 15-70 μg/kg/hour;

said second infusion comprises administering an amount of allopregnanolone/unit time of 50-100 μg/kg/hour, 70-100 μg/kg/hour, or 86 μg/kg/hour; and

said third infusion comprising administering a plurality of step doses, wherein each subsequent step dose delivers a lower amount of allopregnanolone/unit time than the step dose that precedes it and the amount of allopregnanolone/unit time is 5-100 μg/kg/hour, 10-80 μg/kg/hour, or 15-70 μg/kg/hour.

8. The method of claim 1 , wherein the allopregnanolone is provided in a composition comprising a cyclodextrin.

9. The method of claim 8 , wherein the cyclodextrin is present in the composition at 1-30% by weight of cyclodextrin per volume of composition.

10. The method of claim 9 , wherein the cyclodextrin is present in the composition at 2-18% by weight of cyclodextrin per volume of composition.

11. The method of claim 1 , wherein the allopregnanolone is provided at a concentration of 0.1 to 10 mg/mL.

12. The method of claim 11 , wherein the allopregnanolone is provided at a concentration of 1 to 5 mg/mL.

13. The method of claim 8 , wherein the cyclodextrin is present in the composition at 2-18% by weight of cyclodextrin per volume of composition, and the allopregnanolone is provided at a concentration of 1 to 5 mg/mL.

14. The method of claim 8 , wherein the cyclodextrin is present in the composition at 1-30% by weight of cyclodextrin per volume of composition, and the allopregnanolone is provided at a concentration of 1 to 5 mg/mL.

15. The method of claim 8 , wherein the cyclodextrin is present in the composition at 25% by weight of cyclodextrin per volume of composition, and the allopregnanolone is provided at a concentration of 5 mg/mL.

16. The method of claim 1 , wherein the infusion is carried out over 60 hours.

Assignments (2)
CHANGE OF NAME Recorded Aug 18, 2026
From: SAGE THERAPEUTICS, INC.
To: SAGE THERAPEUTICS, LLC
Reel/Frame 075866/0450 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 6, 2021
From: KANES, STEPHEN JAY; COLQUHOUN, HELEN
To: SAGE THERAPEUTICS, INC.
Reel/Frame 057179/0667 →
Continuity (5)
Division 15509656
Provisional Application 62213015 · Sep 1, 2015
Provisional Application 62170596 · Jun 3, 2015
Provisional Application 62047599 · Sep 8, 2014
Related Publication 20200253985A1 · Aug 13, 2020
Cited By (4)
US 12,358,942 US 12,473,327 US 12,534,495 US 12,655,175