Dosage regime with esketamine for treating major depressive disorder

Patent metadata

Field	Value
Publication number	US-12268658-B2
Application number	US-202017789631-A
Country	US
Kind code	B2
Filing date	Dec 29, 2020
Priority date	Dec 30, 2019
Publication date	Apr 8, 2025
Grant date	Apr 8, 2025

Abstract

The present invention provides a method for safe and efficacious administration of esketamine.

First claim

What is claimed:

1. A method of treating major depressive disorder (MDD) in a human patient in need thereof with a once daily esketamine administration comprising orally administering to said patient, once every 24 hours, an immediate release oral dosage form comprising between about 41 mg and about 80 mg of esketamine over a treatment regimen of at least 28 days and wherein the esketamine C max of said administration is 30 ng/ml or less and/or the esketamine AUC 0-t of said administration is 60 ng*h/ml or less.

2. The method of claim 1 , wherein the oral dosage form comprises about 45 mg of esketamine.

3. The method of claim 1 , wherein the oral dosage form comprises about 50 mg of esketamine.

4. The method of claim 1 , wherein the oral dosage form comprises about 55 mg of esketamine.

5. The method of claim 1 , wherein the oral dosage form comprises about 60 mg of esketamine.

6. The method of claim 1 , wherein the oral dosage form comprises about 65 mg of esketamine.

7. The method of claim 1 , wherein the oral dosage form comprises about 70 mg of esketamine.

8. The method of claim 1 , wherein the oral dosage form comprises about 75 mg of esketamine.

9. The method of claim 1 , wherein the oral dosage form comprises about 80 mg of esketamine.

10. The method of claim 1 , wherein the treatment regimen is between 28 days and about 730 days.

11. The method of claim 10 , wherein the treatment regimen is between 28 days and about 365 days.

12. The method of claim 1 , wherein the treatment regimen results in a reduction of the symptoms of major depressive disorder (MDD) after at least 28 days of treatment.

13. The method of claim 1 , further comprising the administration of a second medication other than (R)-ketamine.

14. The method of claim 13 , wherein the second medication is an antidepressant, an antimanic agent, or an anxiolytic drug.

15. The method of claim 14 , wherein the antidepressant is selected from the group consisting of fluoxetine, sertraline, paroxetine, citalopram, escitalopram, venlafaxine, desvenlafaxine, duloxetine, and fluvoxamine.

16. The method of claim 1 , wherein the esketamine is esketamine hydrochloride.

17. The method of claim 1 , wherein the esketamine C max of said administration is 30 ng/ml or less.

18. The method of claim 1 , wherein the esketamine AUC 0-t of said administration is 60 ng*h/ml or less.

19. The method of claim 1 , wherein the esketamine C max of said administration is 30 ng/ml or less and the esketamine AUC 0-t of said administration is 60 ng*h/ml or less.

Assignees

• Clexio Biosciences Ltd

Inventors

• Schumann Johanna
• Mimrod Dorit

Classifications

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K31/4525

  containing a five-membered ring with oxygen as a ring hetero atom · CPC title

• A61K31/381

  having five-membered rings · CPC title

• A61K31/343

  condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone · CPC title

• A61K31/15

  Oximes (>C=N—O—); Hydrazines (>N—N<); Hydrazones (>N—N=) {; Imines (C—N=C)} · CPC title