IP Library Granted Patent US 11,273,158
Granted Patent B2
US 11,273,158 · App. 16/291,768 · Granted Mar 15, 2022

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 11,273,158
App. No.
16/291,768
Granted
Mar 15, 2022
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 (41)

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 ; and

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

wherein all components of the method are administered at substantially the same time.

2. The method of claim 1 , wherein the AL NCD of the second component comprises polysorbate 20, sodium citrate, sodium chloride, an aqueous buffer, and a population of particles of aripiprazole lauroxil.

3. The method of claim 2 , wherein the population of particles of aripiprazole lauroxil of the second component has a volume-based particle distribution size (Dv50) between about 175 nm and about 350 nm.

4. The method of claim 2 , wherein the AL NCD has a ratio of particles to polysorbate 20 of 17:1.

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

6. The method of claim 1 , wherein the second component is administered at a dosage of about 675 mg of the active component.

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

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

9. 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, and wherein the first component is not administered again within 21 days of the initial administration.

10. 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.

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

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

13. The method of claim 1 , wherein the first component is only administered on the first and second day of treatment.

14. The method of claim 1 , wherein the first component is only administered on the first day of treatment.

15. 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 ; 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 all components of the method are administered at substantially the same time.

16. The method of claim 15 , wherein the therapeutically effective mean blood plasma level of aripiprazole is about 102-435 ng/mL at steady-state plasma level.

17. The method of claim 15 , wherein the AL NCD of the second component comprises polysorbate 20, sodium citrate, sodium chloride, an aqueous buffer, and a population of particles of aripiprazole lauroxil.

18. The method of claim 17 , wherein the population of particles of aripiprazole lauroxil of the second component have a volume-based particle distribution size (Dv50) between about 175 nm and about 350 nm.

19. The method of claim 17 , wherein the AL NCD has a ratio of particles to polysorbate 20 of 17:1.

20. The method of claim 15 , wherein the therapeutically effective mean blood plasma level of aripiprazole is reached within 24 hours of the initial treatment.

21. The method of claim 15 , wherein the therapeutically effective mean blood plasma level of aripiprazole is maintained for no less than 21 days.

22. The method of claim 15 , wherein the method comprises a regimen wherein the first, second, and third components are administered at substantially the same time, and wherein the first component is not administered again within 21 days of the initial administration.

23. The method of claim 15 , 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.

24. The method of claim 15 , wherein the first component is only administered once during the treatment duration.

25. The method of claim 15 , wherein the first component is not administered again within 21 days following the initial treatment.

26. The method of claim 15 , wherein the first component is only administered on the first and second day of treatment.

27. The method of claim 15 , wherein the first component is only administered on the first day of treatment.

28. The method of claim 1 , wherein

the first component comprises about 30 mg of aripiprazole;

the second component comprises about 629-695 mg of AL NCD ; and

the third component comprises about 662 mg of aripiprazole lauroxil; and

wherein the method comprises a regimen wherein the first component is administered once within the first 21 days of the regimen.

Assignments (7)
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 Feb 13, 2026
From: ALKERMES PHARMA IRELAND LIMITED
To: JPMORGAN CHASE BANK, N.A. AS ADMINISTRATIVE AGENT
Reel/Frame 074858/0405 →
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 13, 2021
From: VON MOLTKE, LISA L.; WEIDEN, PETER J.; HARD, MARJIE L.
To: ALKERMES PHARMA IRELAND LIMITED
Reel/Frame 057168/0420 →
SECURITY INTEREST Recorded Mar 20, 2020
From: ALKERMES PHARMA IRELAND LIMITED
To: MORGAN STANLEY SENIOR FUNDING, INC.
Reel/Frame 052914/0832 →
Continuity (2)
Provisional Application 62638587 · Mar 5, 2018
Related Publication 20190298716A1 · Oct 3, 2019
Cited By (5)
US 12,251,381 US 12,311,027 US 12,629,366 US 12,653,822 US 12,691,056