# US 11,896,563 B2 · Bupropion and dextromethorphan for reduction of suicide risk in depression patients

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- Number: US 11,896,563 B2
- Document ID: US11896563B2
- Status: Granted
- Kind: B2
- Application number: 18/323,714
- Filed: 2023-05-25
- Published: 2023-09-21
- Granted: 2024-02-13
- Earliest claimed: 2020-12-01
- Assignees: Antecip Bioventures II LLC
- Applicants: Antecip Bioventures II LLC
- Inventors: Herriot Tabuteau
- Web page: https://patentgrep.com/patent/US11896563B2

## CPC

- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 31/485: Morphinan derivatives, e.g. morphine, codeine
- A61P 25/24: Antidepressants
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This disclosure relates to a method of treating depression and/or reducing risk of suicide, comprising administering a combination of about 90 mg to about 120 mg of bupropion hydrochloride, or a molar equivalent amount of another form of bupropion, and about 40 mg to about 50 mg of dextromethorphan hydrobromide, or a molar equivalent amount of another form of dextromethorphan. The combination may be administered twice a day to a human being suffering from major depressive disorder and having a score of 3 or greater on the Suicidality Item of the Montgomery-Åsberg Depression Rating Scale (MADRS-SI).

## Claims

### Claim 1

A method of treating depression and reducing risk of suicide, comprising: selecting a human being suffering from major depressive disorder and having a score of 3 or greater on the Suicidality Item of the Montgomery-Åsberg Depression Rating Scale (MADRS-SI), and administering a combination of about 90 mg to about 120 mg of bupropion hydrochloride, or a molar equivalent amount of another form of bupropion, and about 40 mg to about 50 mg of dextromethorphan hydrobromide, or a molar equivalent amount of another form of dextromethorphan, to the human being; wherein the combination is administered twice a day to the human being.

### Claim 2 (depends on 1)

The method of claim 1, wherein the combination comprises about 105 mg of bupropion hydrochloride, or a molar equivalent amount of another form of bupropion, and about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of another form of dextromethorphan.

### Claim 3 (depends on 1)

The method of claim 1, wherein the combination is administered twice a day for at least one week.

### Claim 4 (depends on 3)

The method of claim 3, wherein the combination is administered twice a day for at least two weeks.

### Claim 5 (depends on 4)

The method of claim 4, wherein the combination is administered twice a day for at least six weeks.

### Claim 6 (depends on 1)

The method of claim 1, wherein the MADRS-SI of the human being is reduced by at least 30% after the combination is administered to the human being twice a day for one week.

### Claim 7 (depends on 1)

The method of claim 1, wherein the MADRS-SI of the human being is reduced by at least 50% after the combination is administered to the human being twice a day for two weeks.

### Claim 8 (depends on 1)

The method of claim 1, wherein the MADRS-SI of the human being is reduced by at least 60% after the combination is administered to the human being twice a day for four weeks.

### Claim 9 (depends on 1)

The method of claim 1, wherein after eight days of administration of the combination twice a day, the Cmax of dextromethorphan in the human being is increased about 15-fold to about 25-fold as compared to a single administration of the combination.

### Claim 10 (depends on 1)

The method of claim 1, wherein after eight days of administering the combination twice a day, the Cmin of dextromethorphan in the human being is increased about 35-fold to about 45-fold as compared to a single administration of the combination.

### Claim 11 (depends on 1)

The method of claim 1, wherein after eight days of administering the combination twice a day, the AUC0-12 of dextromethorphan in the human being is increased about 25-fold to about 45-fold as compared to a single administration of the combination.

### Claim 12 (depends on 2)

The method of claim 2, wherein after eight days of administering the combination twice a day, the Cmax of dextromethorphan in the human being is about 75 ng/mL to about 80 ng/mL.

### Claim 13 (depends on 2)

The method of claim 2, wherein after eight days of administering the combination twice a day, the Cmin of dextromethorphan is about 42 ng/mL to about 50 ng/mL.

### Claim 14 (depends on 2)

The method of claim 2, wherein after eight days of administering the combination twice a day, the AUC0-12 of dextromethorphan in the human being is about 755 ng·hr/mL.

### Claim 15 (depends on 2)

The method of claim 2, wherein after eight days of administering the combination twice a day, the Cmax of bupropion in the human being is about 85 ng/mL to about 90 ng/mL.

### Claim 16 (depends on 2)

The method of claim 2, wherein after eight days of administering the combination twice a day, the Cmin of bupropion is about 25 ng/mL to about 35 ng/mL.

### Claim 17 (depends on 2)

The method of claim 2, wherein after eight days of administering the combination twice a day, the AUC0-12 of bupropion in the human being is about 660 ng·hr/mL to about 670 ng·hr/mL.
