Granted Patent B2

US 12,364,674 · App. 18/541,574 · Granted Jul 22, 2025

Inventor: Herriot Tabuteau (New York, NY)

Assignee: ANTECIP BIOVENTURES II LLC

A61K31/137A61K9/2009A61K9/2013A61K9/2027A61K9/2054A61K9/2086A61K31/135A61K31/4525A61K31/485A61P25/24G01N33/942A61K9/20G01N2800/52

Abstract

Claims (25)

1. A method of treating agitation associated with Alzheimer's disease in a human patient who requires concomitant treatment with a strong CYP2D6 inhibitor, comprising administering, once daily to the human patient, a combination of about 105 mg of bupropion hydrochloride and about 45 mg of dextromethorphan hydrobromide, wherein the human patient is experiencing agitation associated with Alzheimer's disease and is receiving concomitant treatment with the strong CYP2D6 inhibitor, wherein the dextromethorphan and the bupropion are the only active agents in the combination, and wherein the strong CYP2D6 inhibitor is paroxetine.

2. The method of claim 1 , wherein the combination of about 105 mg of bupropion hydrochloride and about 45 mg of dextromethorphan hydrobromide is present in a solid oral dosage form.

3. The method of claim 2 , wherein the once-daily administration avoids the human patient having an about 2.7-fold increase in AUC 0-12 of dextromethorphan as compared to the AUC 0-12 of dextromethorphan that would result after 8 days of twice daily administration of the solid dosage form to the human patient without the concomitant treatment with the strong CYP2D6 inhibitor.

4. The method of claim 2 , wherein the once-daily administration avoids the patient having an about 2.4-fold increase in C max of dextromethorphan as compared to the C max of dextromethorphan that would result after 8 days of twice daily administration of the solid dosage form to the human patient without the concomitant treatment with the strong CYP2D6 inhibitor.

5. The method of claim 2 , wherein the solid dosage form is orally administered in the morning.

6. The method of claim 5 , wherein the dextromethorphan is in an immediate-release formulation.

7. The method of claim 6 , wherein the bupropion is in an extended-release formulation.

8. The method of claim 7 , wherein the once-daily administration avoids the human patient having an about 2.7-fold increase in AUC 0-12 of dextromethorphan as compared to the AUC 0-12 of dextromethorphan that would result after 8 days of twice daily administration of the solid dosage form to the human patient without the concomitant treatment with the strong CYP2D6 inhibitor.

9. The method of claim 7 , wherein the once-daily administration avoids the patient having an about 2.4-fold increase in C max of dextromethorphan as compared to the C max of dextromethorphan that would result after 8 days of twice daily administration of the solid dosage form to the human patient without the concomitant treatment with the strong CYP2D6 inhibitor.

10. The method of claim 7 , wherein the solid dosage form further contains a carbomer homopolymer.

11. The method of claim 7 , wherein the solid dosage form further contains colloidal silicon dioxide.

12. The method of claim 7 , wherein the solid dosage form further contains crospovidone.

13. The method of claim 7 , wherein the solid dosage form further contains glyceryl monocaprylocaprate.

14. The method of claim 7 , wherein the solid dosage form further contains L-cysteine hydrochloride monohydrate.

15. The method of claim 7 , wherein the solid dosage form further contains magnesium stearate.

16. The method of claim 7 , wherein the solid dosage form further contains microcrystalline cellulose.

17. The method of claim 7 , wherein the solid dosage form further contains polyvinyl alcohol.

18. The method of claim 7 , wherein the solid dosage form further contains red iron oxide.

19. The method of claim 7 , wherein the solid dosage form further contains sodium lauryl sulfate.

20. The method of claim 7 , wherein the solid dosage form further contains stearic acid.

21. The method of claim 7 , wherein the solid dosage form further contains talc.

22. The method of claim 7 , wherein the solid dosage form further contains titanium dioxide.

23. The method of claim 7 , wherein the solid dosage form further contains yellow iron oxide.

24. The method of claim 7 , wherein administration of the solid dosage form twice daily to the human patient for 8 days would result in the human patient having about the same AUC 0-12 of bupropion as compared to the AUC 0-12 of bupropion that would result after 8 days of twice daily administration of the solid dosage form to a human patient without the concomitant treatment with the strong CYP2D6 inhibitor.

25. The method of claim 7 , wherein administration of the solid dosage form twice daily to the human patient for 8 days would result in the human patient having about the same C max of bupropion as compared to the C max of bupropion that would result after 8 days of twice daily administration of the solid dosage form to a human patient without the concomitant treatment with the strong CYP2D6 inhibitor.

Assignments (1)

Continuity (8)

References Cited (400)

Cited By (8)

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