Dosage regime with esketamine for treating neuropsychiatric or neurological conditions

Patent metadata

Field	Value
Publication number	US-12478592-B2
Application number	US-202017789648-A
Country	US
Kind code	B2
Filing date	Dec 29, 2020
Priority date	Dec 30, 2019
Publication date	Nov 25, 2025
Grant date	Nov 25, 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 a condition other than major depressive disorder (MDD) in a human patient in need thereof comprising orally administering once-daily to said patient an immediate release oral dosage form comprising esketamine over a treatment regimen of at least 28 days, and wherein
a. the esketamine C max of said administration is 30 ng/ml or less, or b. the esketamine AUC 0-t of said administration is 60 ng*h/ml or less, or c. the esketamine C max of said administration is 30 ng/ml or less and the AUC 0-t of said administration is 60 ng*h/ml or less.

2 . The method of claim 1 , wherein the condition is selected from the group consisting of acute stress disorder, alcohol dependence disorder, alcohol use disorder, anorexia nervosa, anxiety disorders, bipolar disorder, borderline personality disorder, bulimia nervosa, PMDD, schizoaffective disorder, ALS, Alzheimer's disease, chronic fatigue, diabetic neuropathy, dyskinesia, fibromyalgia, opioid tolerance, pain and traumatic brain injury and schizophrenia.

3 . The method of claim 2 , wherein the anxiety disorder is selected from the group consisting of Generalized Anxiety Disorder, Social Anxiety Disorder, agoraphobia, Panic Disorder and phobias.

4 . The method of claim 1 , wherein the oral dosage form comprises about 40 mg of esketamine.

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

6 . The method of claim 5 , wherein the treatment regimen is between 28 days and about 365 days.

7 . The method of claim 1 , wherein the treatment regimen results in a reduction of the symptoms of the condition other than major depressive disorder after at least 28 days of treatment.

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

9 . The method of claim 8 , wherein the second medication is an antidepressant an anticonvulsant, an antipsychotic, a mood stabilizer, an anxiolytic or an antimanic agent.

10 . 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.

11 . The method of claim 10 , wherein the esketamine C max of said administration is 15 ng/ml or less and/or the esketamine AUC 0-t of said administration is 30 ng*h/ml or less.

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

13 . A method of treating a condition other than major depressive disorder in a human patient in need thereof comprising once-daily orally administering to said patient an immediate release oral dosage form comprising esketamine, and wherein said dosage form provides for an (S)-norketamine C max of between 15 and 150 ng/ml and/or an (S)-norketamine AUC 0-t of between 105 and 850 ng*h/ml.

14 . The method of claim 13 , comprising orally administering to said patient a dosage form, wherein said dosage form provides for an(S)-norketamine C max of between 15 and 150 ng/ml and an (S)-norketamine AUC 0-t of between 105 and 850 ng*h/ml.

15 . A method of treating a condition other than major depressive disorder in a human patient in need thereof comprising once-daily orally administering to said patient an immediate release oral dosage form comprising esketamine, and wherein said dosage form provides for an (2S,6S)—OH-norketamine C max of between 15 and 75 ng/ml and/or an (2S,6S)—OH-norketamine AUC 0-t of between 105 and 850 ng*h/ml.

16 . The method of claim 15 , comprising orally administering to said patient a dosage form, wherein said dosage form provides for an (2S,6S)—OH-norketamine C max of between 15 and 75 ng/ml and an (2S,6S)—OH-norketamine AUC 0-t of between 105 and 850 ng*h/ml.

Assignees

• Clexio Biosciences Ltd

Inventors

• Gershon Ari
• Dangoor David

Classifications

• A61K45/06

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

• A61P25/22

  Anxiolytics · CPC title

• A61P25/02

  for peripheral neuropathies · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title

• A61K31/343

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