Granted Patent B2

US 12,194,005 · App. 18/422,531 · Granted Jan 14, 2025

Inventor: Herriot Tabuteau (New York, NY)

Assignee: ANTECIP BIOVENTURES II LLC

A61K31/137A61K9/2009A61K9/2013A61K9/2027A61K9/2054A61K9/2086A61K31/4525A61K31/485A61P25/24

Abstract

Claims (19)

1. A method of treating agitation associated with Alzheimer's disease, comprising: selecting a human patient for having: 1) moderate renal impairment and 2) agitation associated with Alzheimer's disease, wherein the human patient orally receives a maximum of one tablet once daily, wherein the tablet contains about 105 mg of bupropion hydrochloride and about 45 mg of dextromethorphan hydrobromide, wherein the human patient has an estimated glomerular filtration rate that is between 30 mL/min/1.73 m 2 and 59 mL/min/1.73 m 2 , wherein the dextromethorphan hydrobromide is in an immediate-release formulation, wherein the bupropion hydrochloride is in an extended-release formulation, and wherein the tablet is a bilayer tablet.

2. The method of claim 1 , wherein the tablet is swallowed whole by the human patient.

3. The method of claim 1 , wherein after the human patient has orally received one tablet daily for 8 days, steady state plasma concentrations of dextromethorphan and bupropion in the human patient are achieved, and wherein the accumulation ratio for dextromethorphan at steady state is about 20 based on the C max .

4. The method of claim 1 , wherein after the human patient has orally received one tablet daily for 8 days, steady state plasma concentrations of dextromethorphan and bupropion in the human patient are achieved, and wherein the accumulation ratio for dextromethorphan at steady state is about 32 based on the AUC 0-12 .

5. The method of claim 1 , wherein the once-daily administration of the tablet avoids the human patient having an about 2.2-fold increase in AUC 0-12 of dextromethorphan as compared to the AUC 0-12 of dextromethorphan that would result from twice daily administration of the tablet for 8 days to a human patient who has no renal impairment.

6. The method of claim 1 , wherein the once-daily administration of the tablet avoids the human patient having an about 2.1-fold increase in C max of dextromethorphan as compared to the C max of dextromethorphan that would result from twice daily administration of the tablet for 8 days to a human patient who has no renal impairment.

7. The method of claim 1 , wherein the once-daily administration of the tablet avoids the human patient having an about 1.8-fold increase in AUC 0-12 of bupropion as compared to the AUC 0-12 of bupropion that would result from twice daily administration of the tablet for 8 days to a human patient who has no renal impairment.

8. The method of claim 1 , wherein the once-daily administration of the tablet avoids the human patient having an about 1.9-fold increase in C max of bupropion as compared to the C max of bupropion that would result from twice daily administration of the tablet for 8 days to a human patient who has no renal impairment.

9. The method of claim 1 , wherein the T max of dextromethorphan is about 3 hours.

10. A method of treating agitation associated with Alzheimer's disease, comprising: selecting a human patient for having: 1) moderate renal impairment and 2) agitation associated with Alzheimer's disease, wherein the human patient orally receives a maintenance dose of one tablet once daily, wherein the tablet contains about 105 mg of bupropion hydrochloride and about 45 mg of dextromethorphan hydrobromide, wherein the dextromethorphan hydrobromide is in an immediate-release formulation, wherein the bupropion hydrochloride is in an extended-release formulation, and wherein the tablet is a bilayer tablet.

11. The method of claim 10 , wherein the tablet is swallowed whole by the human patient.

12. The method of claim 10 , wherein after the human patient has orally received one tablet daily for 8 days, steady state plasma concentrations of dextromethorphan and bupropion are achieved in the human patient, and wherein the accumulation ratio for dextromethorphan at steady state is about 20 based on the C max .

13. The method of claim 10 , wherein after the human patient has orally received one tablet daily for 8 days, steady state plasma concentrations of dextromethorphan and bupropion are achieved in the human patient, and wherein the accumulation ratio for dextromethorphan is about 32 based on the AUC 0-12 .

14. The method of claim 10 , wherein the once-daily administration of the tablet avoids the human patient having an about 2.2-fold increase in AUC 0-12 of dextromethorphan as compared to the AUC 0-12 of dextromethorphan that would result from twice daily administration of the tablet for 8 days to a human patient who has no renal impairment.

15. The method of claim 10 , wherein the once-daily administration of the tablet avoids the human patient having an about 2.1-fold increase in C max of dextromethorphan as compared to the C max of dextromethorphan that would result from twice daily administration of the tablet for 8 days to a human patient who has no renal impairment.

16. The method of claim 10 , wherein the once-daily administration of the tablet avoids the human patient having an about 1.8-fold increase in AUC 0-12 of bupropion as compared to the AUC 0-12 of bupropion that would result from twice daily administration of the tablet for 8 days to a human patient who has no renal impairment.

17. The method of claim 10 , wherein the once-daily administration of the tablet avoids the human patient having an about 1.9-fold increase in C max of bupropion as compared to the C max of bupropion that would result from twice daily administration of the tablet for 8 days to a human patient who has no renal impairment.

18. The method of claim 10 , wherein the human patient has an estimated glomerular filtration rate that is between 30 ml/min/1.73 m 2 and 59 mL/min/1.73 m 2 .

19. The method of claim 10 , wherein the T max of dextromethorphan is about 3 hours.

Assignments (1)

Continuity (8)

References Cited (400)

Cited By (19)

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