# US 2024/0197754 A1 · Anticonvulsant activity of steroids

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- Number: US 2024/0197754 A1
- Document ID: US20240197754A1
- Status: Published application
- Kind: A1
- Application number: 18/442,086
- Filed: 2024-02-14
- Published: 2024-06-20
- Earliest claimed: 2012-11-30
- Assignees: The Regents of the University of California
- Applicants: The Regents of the University of California
- Inventors: MICHAEL A. ROGAWSKI; Dorota ZOLKOWSKA
- Web page: https://patentgrep.com/patent/US20240197754A1

## CPC

- A61K 31/57: substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61K 47/40: Cyclodextrins; Derivatives thereof
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 25/28: 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
- A61P 25/32: Alcohol-abuse
- A61P 25/34: Tobacco-abuse
- 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

The present invention relates to methods of preventing, inhibiting, delaying. and/or mitigating seizures by administration of a steroid, e.g., a neurosteroid, e.g., allopregnanolone.

## Claims

### Claim 1

A method of treating, reducing, and/or mitigating symptoms associated with and/or caused by traumatic brain injury, Alzheimer's disease, epilepsy, anxiety, fragile X syndrome, post-traumatic stress disorder, lysosomal storage disorders (Niemann-Pick type C disease), depression (including post-partum depression), premenstrual dysphoric disorder, alcohol craving, and smoking cessation in a subject in need thereof, comprising administration to the subject a steroid.

### Claim 2

A method of treating, reducing, and/or mitigating symptoms associated with and/or caused by epilepsy, in a subject in need thereof, comprising administration to the subject a steroid.

### Claim 3

A method of accelerating the termination or abortion of an impending seizure in a subject in need thereof, comprising administration to the subject a steroid.

### Claim 4 (depends on 1, 2, 3)

The method of any one of claims 1 to 3, wherein the steroid is a neurosteroid.

### Claim 5 (depends on 1, 2, 3, 4)

The method of any one of claims 1 to 4, wherein the neurosteroid is selected from the group consisting of allopregnanolone, allotetrahydrodeoxycorticosterone, ganaxolone, alphaxolone, alphadolone, hydroxydione, minaxolone, and Althesin.

### Claim 6 (depends on 5)

The method of claim 5, wherein the neurosteroid is allopregnanolone.

### Claim 7 (depends on 5, 6)

The method of any one of claims 5 to 6, wherein the steroid is formulated in a cyclodextrin.

### Claim 8 (depends on 1, 2, 3, 4, 5, 6, 7)

The method of any one of claims 1 to 7, wherein the steroid is formulated in hydroxypropyl-beta-cyclodextrin, sulfobutylether-beta-cyclodextrin sodium salt, or a mixture thereof.

### Claim 9 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

The method of any one of claims 1 to 8, wherein the subject is experiencing aura.

### Claim 10 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9)

The method of any one of claims 1 to 9, wherein the subject has been warned of an impending seizure.

### Claim 11 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10)

The method of any one of claims 1 to 10, wherein the subject is experiencing a seizure.

### Claim 12 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11)

The method of any one of claims 1 to 11, wherein the subject has status epilepticus.

### Claim 13 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11)

The method of any one of claims 1 to 11, wherein the subject has myoclonic epilepsy.

### Claim 14 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11)

The method of any one of claims 1 to 11, wherein the subject suffers from seizure clusters.

### Claim 15 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14)

The method of any one of claims 1 to 14, wherein the seizure is a tonic seizure.

### Claim 16 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14)

The method of any one of claims 1 to 14, wherein the seizure is a clonic seizure.

### Claim 17 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)

The method of any one of claims 1 to 16, wherein the subject is a human.

### Claim 18 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17)

The method of any one of claims 1 to 17, wherein the steroid is administered intramuscularly (i.m.), subcutaneously (s.c.) or intravenously (i.v.).

### Claim 19 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)

The method of any one of claims 1 to 18, wherein the steroid is administered at a dose in the range of about 0.25 mg/kg to about 15 mg/kg.

### Claim 20 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19)

The method of any one of claims 1 to 19, comprising treating, reducing, and/or mitigating symptoms associated with and/or caused by epilepsy by intramuscularly (i.m.), subcutaneously (s.c.) or intravenously (i.v.) administering allopregnanolone formulated in a sulfobutylether-beta-cyclodextrin sodium salt.

### Claim 21 (depends on 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)

The method of any one of claims 1 to 20, wherein the epilepsy is status epilepticus.

### Claim 22

A composition comprising or consisting essentially of a steroid and a cyclodextrin.

### Claim 23 (depends on 22)

The composition of claim 22, wherein the steroid is a neurosteroid.

### Claim 24 (depends on 23)

The composition of claim 23, wherein the neurosteroid is selected from the group consisting of allopregnanolone, allotetrahydrodeoxycorticosterone, ganaxolone, alphaxolone, alphadolone, hydroxydione, minaxolone, and Althesin.

### Claim 25 (depends on 22, 23, 24)

The composition of any one of claims 22 to 24, wherein the steroid is allopregnanolone.

### Claim 26 (depends on 22, 23, 24, 25)

The composition of any one of claims 22 to 25, wherein the cyclodextrin is hydroxypropyl-beta-cyclodextrin, sulfobutylether-beta-cyclodextrin sodium salt, or a mixture thereof.

### Claim 27 (depends on 22, 23, 24, 25, 26)

The composition of any one of claims 22 to 26, wherein the composition is formulated for intramuscular (i.m.), subcutaneous (s.c.) or intravenous (i.v.) administration.

### Claim 28 (depends on 22, 23, 24, 25, 26, 27)

The composition of any one of claims 22 to 27, wherein the composition comprises allopregnanolone and sulfobutylether-beta-cyclodextrin sodium salt.