IP Library Granted Patent US 12,251,381
Granted Patent B2
US 12,251,381 · App. 17/665,015 · Granted Mar 18, 2025

Aripiprazole dosing strategy

Inventors: Lisa L. von Moltke (Newton, MA); Peter J. Weiden (Newton, MA); Marjie L. Hard (Lexington, MA)
Assignee: Alkermes Pharma Ireland Limited
A61K31/497A61K31/496A61K47/02A61K47/12A61K47/26A61P25/18A61K9/0019A61K9/0053
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Quick Facts
Patent No.
US 12,251,381
App. No.
17/665,015
Granted
Mar 18, 2025
Kind
B2
Abstract

The present invention relates to methods of treating schizophrenia using a combination of aripiprazole, aripiprazole lauroxil, and a nanoparticle dispersion of aripiprazole lauroxil.

Claims (36)

1. A method of treating schizophrenia in a subject in need thereof, the method comprising administering to the subject:

a first component comprising about 5-50 mg of aripiprazole;

a second component comprising about 629-695 mg of AL NCD having a volume-based particle distribution size (Dv50) between about 175 nm and about 350 nm; and

a third component comprising a therapeutically effective amount of aripiprazole lauroxil;

wherein the method comprises a regimen wherein the first component is only administered on the first and/or second days of treatment, the second component is only administered on the first day of treatment, and the third component is only administered once within the first 10 days of treatment.

2. The method of claim 1 , wherein the AL NCD comprises polysorbate 20, sodium citrate, sodium chloride, an aqueous buffer, and a population of particles of aripiprazole lauroxil, wherein the AL NCD has a ratio of particles to polysorbate 20 of between about 0.1:1 and about 40:1.

3. The method of claim 1 , wherein the first component is administered at a dosage of about 30 mg or about 15 mg.

4. The method of claim 1 , wherein the second component is administered at a dosage of about 675 mg of AL NCD .

5. The method of claim 1 , wherein the third component is administered at a dosage of about 300-1500 mg.

6. The method of claim 1 , wherein the third component is administered at a dosage of 441, 662, 882, or 1064 mg.

7. The method of claim 1 , wherein the method comprises a regimen wherein the first, second, and third components are administered at substantially the same time, followed by a second treatment comprising administering the third component alone.

8. The method of claim 7 , wherein the second treatment occurs no earlier than 21 days after the initial treatment.

9. The method of claim 1 , wherein the first component is only administered once during the treatment duration.

10. The method of claim 1 , wherein the first component is not administered again within 21 days following the initial treatment.

11. The method of claim 9 , wherein the third component is administered on the first or second day of treatment.

12. The method of claim 9 , wherein the third component is administered 7-10 days after the start of the treatment regimen.

13. The method of claim 9 , wherein the first component is only administered on the first day of treatment.

14. The method of claim 1 , wherein the first component is administered orally.

15. The method of claim 1 , wherein the second component and third component are administered intra-muscularly to the deltoid or gluteus.

16. A method of treating schizophrenia in a subject in need thereof, the method comprising administering to the subject:

a first component comprising aripiprazole;

a second component comprising AL NCD having a volume-based particle distribution size (Dv50) between about 175 nm and about 350 nm; and

a third component comprising aripiprazole lauroxil;

wherein the dosages of the first, second, and third components combined are sufficient to maintain a therapeutically effective mean blood plasma level of aripiprazole in the subject; and

wherein the method comprises a regimen wherein the first component is only administered on the first and/or second days of treatment, the second component is only administered on the first day of treatment, and the third component is only administered once within the first 10 days of treatment.

17. The method of claim 16 , wherein the AL NCD comprises polysorbate 20, sodium citrate, sodium chloride, an aqueous buffer, and a population of particles of aripiprazole lauroxil, wherein the AL NCD has a ratio of particles to polysorbate 20 of between about 0.1:1 and about 40:1.

18. The method of claim 16 , wherein the therapeutically effective mean blood plasma level of aripiprazole is reached within 24 hours of the initial treatment.

19. The method of claim 16 , wherein the therapeutically effective mean blood plasma level of aripiprazole is maintained for no less than 21 days.

20. The method of claim 16 , wherein the first component is only administered once during the treatment duration.

21. The method of claim 16 , wherein the first component is not administered again within 21 days following the initial treatment.

22. The method of claim 16 , wherein the regimen further comprises a second administration of the third component alone.

23. The method of claim 16 , wherein the third component is administered on the first or second day of treatment.

24. The method of claim 16 , wherein the third component is administered 7-10 days after the start of the treatment regimen.

25. The method of claim 16 , wherein the first component is only administered on the first day of treatment.

26. The method of claim 16 , wherein the first component is administered orally.

27. The method of claim 16 , wherein the second component and third component are administered intra-muscularly to the deltoid or gluteus.

Assignments (6)
SECURITY INTEREST Recorded Feb 13, 2026
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 074858/0405 →
RELEASE OF SECURITY INTEREST IN PATENTS PREVIOUSLY RECORDED AT REEL/FRAME (073213/0302) Recorded Feb 13, 2026
From: JPMORGAN CHASE BANK, N.A., AS ADMINISTRATIVE AGENT
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 074858/0429 →
SECURITY INTEREST Recorded Oct 23, 2025
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 073213/0302 →
RELEASE OF PATENT SECURITY AGREEMENTS Recorded Dec 24, 2024
From: MORGAN STANLEY SENIOR FUNDING, INC.
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 069771/0701 →
SECURITY AGREEMENT Recorded Jul 17, 2023
From: ALKERMES PHARMA IRELAND LIMITED
To: MORGAN STANLEY SENIOR FUNDING, INC.
Reel/Frame 064286/0821 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 3, 2022
From: VON MOLTKE, LISA L.; WEIDEN, PETER J.; HARD, MARJIE L.
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 060711/0486 →