# US 11,439,612 B2 · Formulations for administration of eflornithine

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- Number: US 11,439,612 B2
- Document ID: US11439612B2
- Status: Granted
- Kind: B2
- Application number: 17/002,117
- Filed: 2020-08-25
- Published: 2021-02-11
- Granted: 2022-09-13
- Earliest claimed: 2016-10-06
- Assignees: Orbus Therapeutics, Inc.
- Applicants: Orbus Therapeutics, Inc.
- Inventors: Victor A. Levin; Noymi Yam; Alexander Vakoula
- Web page: https://patentgrep.com/patent/US11439612B2

## CPC

- A61K 31/18: Sulfonamides (compounds containing a para-N-benzene-sulfonyl-N- group A61K31/63)
- A61K 31/197: the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid (carnitine A61K31/205)
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/0095: {Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006)}
- A61K 31/17: having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine (isoureas, isothioureas A61K31/155; sulfonylureas A61K31/64)
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 229/00: Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

Eflornithine is an agent that can be used to treat glioma, especially glioma of WHO Grade II or Grade III such as anaplastic glioma. Eflornithine can suppress or prevent mutations in glioma which can cause the glioma to progress to a higher grade. The present invention describes pharmaceutical compositions that contain eflornithine or a derivative, analog, or prodrug thereof. The pharmaceutical compositions can be prepared in a number of dosage forms and may contain another therapeutically active agent or an agent that enhances the therapeutic activity of the elformithine or the derivative, analog, or prodrug thereof. The present invention also describes a kit that includes dosage forms of pharmaceutical compositions according to the present invention.

## Claims

### Claim 1

A kit, comprising:
a pouch of solid eflornithine hydrochloride hydrate wherein the pouch comprises an individual dosage of eflornithine hydrochloride hydrate and a pharmaceutically acceptable excipient; and
instructions to prepare an oral solution of eflornithine hydrochloride hydrate.

### Claim 2 (depends on 1)

The kit of claim 1, wherein the instructions describe preparing an eflornithine hydrochloride hydrate oral solution with a concentration of about 13.5 wt % to about 22.5 wt % in water.

### Claim 3 (depends on 1)

The kit of claim 1, wherein the instructions describe preparing an eflornithine hydrochloride hydrate oral solution with a concentration of about 16.2 wt % to about 19.8 wt % in water.

### Claim 4 (depends on 1)

The kit of claim 1, wherein the solid eflornithine hydrochloride hydrate is in the form of a powder.

### Claim 5 (depends on 1)

The kit of claim 1, wherein the solid eflornithine hydrochloride hydrate is in the form of a tablet.

### Claim 6 (depends on 1)

The kit of claim 1, wherein the one or more pouches further comprise a sweetening agent.

### Claim 7 (depends on 6)

The kit of claim 6, wherein the one or more pouches comprise less than 1 wt % of the sweetening agent.

### Claim 8 (depends on 7)

The kit of claim 7, wherein the sweetening agent is selected from the group consisting of an aspartame, dextran, dextrose, fructose, glycerol, mannitol, saccharin, calcium saccharin, sodium saccharin, sorbitol, sucrose, compressible sugar, confectioner's sugar, and syrup.

### Claim 9 (depends on 8)

The kit of claim 8, wherein the sweetening agent is saccharin sodium dihydrate.

### Claim 10 (depends on 1)

The kit of claim 1, wherein the pharmaceutically acceptable excipient is selected from the group consisting of maize starch, wheat starch, rice starch, potato starch, gelatin, gum, methyl cellulose, hydroxypropylmethyl-cellulose, sodium carboxymethylcellulose, or polyvinylpyrrolidone (PVP).

### Claim 11 (depends on 10)

The kit of claim 10, wherein the pharmaceutically acceptable excipient is hydroxypropylmethyl-cellulose or polyvinylpyrrolidone.

### Claim 12 (depends on 1)

The kit of claim 1, further comprising one or more additional pouches of solid eflornithine hydrochloride hydrate wherein each additional pouch comprises an individual dosage of eflornithine hydrochloride hydrate and a pharmaceutically acceptable excipient.

### Claim 13 (depends on 1)

A method of preparing an oral solution of eflornithine hydrochloride hydrate, comprising adding the contents of a pouch of the kit of claim 1 to water according to the instructions to make the oral solution.

### Claim 14 (depends on 1)

A method of treating a subject with anaplastic astrocytoma, comprising administering a dose of an oral solution of eflornithine hydrochloride hydrate prepared with a pouch of the kit of claim 1 to a subject in need thereof.

### Claim 15 (depends on 14)

The method of claim 14, comprising administering to the subject two or more doses of eflornithine hydrochloride hydrate per day.

### Claim 16 (depends on 14)

The method of claim 14, wherein the eflornithine hydrochloride hydrate oral solution is administered for two weeks out of every three weeks.