Granted Patent B2

US 12,433,884 · App. 19/182,463 · Granted Oct 7, 2025

Inventor: Herriot Tabuteau (New York, NY)

Assignee: ANTECIP BIOVENTURES II LLC

A61K31/485A61K9/0053A61K31/135A61K31/137A61K31/15A61K31/343A61K31/381

Abstract

Claims (21)

1. A method of treating agitation associated with Alzheimer's disease in a human being suffering from agitation associated with Alzheimer's disease; comprising orally administering a first tablet once daily for one week followed by twice daily for one week, then a second tablet twice daily to the human being; wherein the first tablet contains about 105 mg of bupropion hydrochloride or a molar equivalent amount of another salt form of bupropion or the free base form of bupropion, and about 30 mg of dextromethorphan hydrobromide or a molar equivalent amount of another salt form of dextromethorphan or the free base form of dextromethorphan; and the second tablet contains about 105 mg of bupropion hydrochloride or a molar equivalent amount of another salt form of bupropion or the free base form of bupropion, and about 45 mg of dextromethorphan hydrobromide or a molar equivalent amount of another salt form of dextromethorphan or the free base form of dextromethorphan; wherein the dextromethorphan and the bupropion are the only therapeutically active agents in the first or second tablet; and wherein the human being is an extensive metabolizer of dextromethorphan.

2. The method of claim 1 , wherein the second tablet is administered twice daily for at least three weeks.

3. The method of claim 1 , wherein the first or second tablet provides immediate release of the dextromethorphan.

4. The method of claim 3 , wherein the first or second tablet provides sustained release of the bupropion.

5. The method of claim 1 , wherein the human being has an age of 65 years to 90 years.

6. The method of claim 1 , wherein the human being has a diagnosis of probable Alzheimer's disease according to the 2011 National Institute on Aging and Alzheimer's Association (NIA-AA) criteria.

7. The method of claim 1 , wherein the human being has a diagnosis of agitation according to the International Psychogeriatric Association (IPA) provisional definition of agitation.

8. The method of claim 1 , wherein the human being has a Mini-Mental State Examination (MMSE) score between 10 and 24.

9. The method of claim 1 , wherein the human being has a Neuropsychiatric Inventory-Agitation and Aggressive domain (NPI-AA) score of 4 or greater.

10. The method of claim 1 , wherein the human being is community dwelling.

11. The method of claim 1 , wherein the human being is not receiving a concomitant selective serotonin reuptake inhibitor.

12. The method of claim 1 , wherein the human being is not receiving a concomitant a serotonin and norepinephrine inhibitor.

13. The method of claim 1 , wherein the human being is not experiencing a dementia of non-Alzheimer's type.

14. The method of claim 1 , wherein the first tablet contains 30 mg of dextromethorphan hydrobromide.

15. The method of claim 14 , wherein the first tablet contains 105 mg of bupropion hydrochloride.

16. The method of claim 1 , wherein the second tablet contains 45 mg of dextromethorphan hydrobromide.

17. The method of claim 16 , wherein the second tablet contains 105 mg of bupropion hydrochloride.

18. The method of claim 1 , wherein the first or second tablet further contains a carbomer homopolymer, colloidal silicon dioxide, crospovidone, glyceryl monocaprylocaprate, magnesium stearate, microcrystalline cellulose, polyvinyl alcohol, red iron oxide, stearic acid, talc, titanium dioxide, yellow iron oxide, or a combination thereof.

19. The method of claim 1 , wherein the first or second tablet further comprises a pharmaceutically acceptable excipient.

20. The method of claim 1 , wherein method is more effective in treating agitation associated with Alzheimer's disease than administering bupropion alone or a placebo.

21. A method of treating agitation associated with Alzheimer's disease in a human being suffering from agitation associated with Alzheimer's disease; comprising orally administering a first tablet once daily for one week followed by twice daily for one week, then a second tablet twice daily to the human being; wherein the first tablet contains 105 mg of bupropion hydrochloride and 30 mg of dextromethorphan hydrobromide; and the second tablet contains 105 mg of bupropion hydrochloride and 45 mg of dextromethorphan hydrobromide; wherein the dextromethorphan hydrobromide and the bupropion hydrochloride are the only therapeutically active agents in the first or second tablet; and wherein the human being is an extensive metabolizer of dextromethorphan.

Assignments (1)

Continuity (7)

References Cited (400)

Cited By (3)

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