# US 2013/0158110 A1 · Therapeutic compositions

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- Number: US 2013/0158110 A1
- Document ID: US20130158110A1
- Status: Published application
- Kind: A1
- Application number: 13/769,821
- Filed: 2013-02-18
- Published: 2013-06-20
- Earliest claimed: 2005-12-16
- Assignees: LEO Laboratories Limited
- Inventors: Marc Barry Brown; Michael Crothers; Tahir Nazir
- Web page: https://patentgrep.com/patent/US20130158110A1

## CPC

- A61K 31/22: of acyclic acids, e.g. pravastatin
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 31/215: of carboxylic acids
- A61K 36/47: Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/32: Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers {, poly(meth)acrylates, or polyvinyl pyrrolidone}
- A61K 47/38: Cellulose; Derivatives thereof
- A61P 35/00: Antineoplastic agents
- 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

Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer.

## Claims

### Claim at position 1

-46. (canceled)

### Claim 47

A method of treating skin cancer in a subject in need thereof, the method comprising topically administering a therapeutically effective amount of a pharmaceutical formulation of ingenol angelate to the skin of the subject, wherein the pharmaceutical formulation comprises ingenol angelate in an amount from about 0.001% to about 0.15% w/w, and wherein at least about 99% of the ingenol angelate is ingenol-3-angelate (isoform ‘b’) and the pharmaceutical formulation has a pH of less than 4.

### Claim 48 (depends on 47)

The method of claim 47, wherein the pharmaceutical formulation has a pH of about 3.5 or less.

### Claim 49 (depends on 47)

The method of claim 47, wherein the pharmaceutical formulation has a pH of about 3.0.

### Claim 50 (depends on 47)

The method of claim 47, wherein the pharmaceutical formulation has a pH within the range of about 2.5 to less than 4.0.

### Claim 51 (depends on 47)

The method of claim 47, wherein the skin cancer is a squamous cell carcinoma.

### Claim 52 (depends on 47)

The method of claim 47, wherein the skin cancer is a basal cell carcinoma.

### Claim 53 (depends on 47)

The method of claim 47, wherein the skin cancer is a malignant melanoma.

### Claim 54 (depends on 47)

The method of claim 47, wherein the pharmaceutical formulation is a gel.

### Claim 55 (depends on 48)

The method of claim 48, wherein the skin cancer is a squamous cell carcinoma.

### Claim 56 (depends on 48)

The method of claim 48, wherein the skin cancer is a basal cell carcinoma.

### Claim 57 (depends on 48)

The method of claim 48, wherein the skin cancer is a malignant melanoma.

### Claim 58 (depends on 48)

The method of claim 48, wherein the pharmaceutical formulation is a gel.

### Claim 59

A method of treating a cancerous skin condition in a subject in need thereof, the method comprising topically administering a therapeutically effective amount of a pharmaceutical formulation of ingenol angelate to the skin of the subject, wherein the pharmaceutical formulation comprises ingenol angelate in an amount from about 0.001% to about 0.15% w/w, and wherein at least about 99% of the ingenol angelate is ingenol-3-angelate (isoform ‘b’) and the pharmaceutical formulation has a pH of less than 4.

### Claim 60 (depends on 59)

The method of claim 59, wherein the pharmaceutical formulation has a pH of about 3.5 or less.

### Claim 61 (depends on 59)

The method of claim 59, wherein the pharmaceutical formulation has a pH of about 3.0.

### Claim 62 (depends on 59)

The method of claim 59, wherein the pharmaceutical formulation has a pH within the range of about 2.5 to less than 4.0.

### Claim 63 (depends on 59)

The method of claim 59, wherein the cancerous skin condition is a squamous cell carcinoma.

### Claim 64 (depends on 59)

The method of claim 59, wherein the cancerous skin condition is a basal cell carcinoma.

### Claim 65 (depends on 59)

The method of claim 59, wherein the cancerous skin condition is a malignant melanoma.

### Claim 66 (depends on 59)

The method of claim 59, wherein the pharmaceutical formulation is a gel.

### Claim 67 (depends on 60)

The method of claim 60, wherein the cancerous skin condition is a squamous cell carcinoma.

### Claim 68 (depends on 60)

The method of claim 60, wherein the cancerous skin condition is a basal cell carcinoma.

### Claim 69 (depends on 60)

The method of claim 60, wherein the cancerous skin condition is a malignant melanoma.

### Claim 70 (depends on 60)

The method of claim 60, wherein the pharmaceutical formulation is a gel.