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Last Updated: September 21, 2021

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Claims for Patent: 9,861,603


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Summary for Patent: 9,861,603
Title:Therapeutic compositions
Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.
Inventor(s): Brown; Marc Barry (Watford, GB), Crothers; Michael Edward Donald (Hillsborough, GB), Nazir; Tahir (Middlesex, GB)
Assignee: LEO Laboratories Limited (Dublin, IE)
Application Number:15/163,454
Patent Claims: 1. 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 comprising ingenol angelate and an acidifying agent to a skin lesion of the subject, at least about 95% of the ingenol angelate being ingenol-3-angelate (isoform `b`); wherein the pharmaceutical formulation comprises ingenol-3-angelate (isoform `b`) in an amount from 0.001% by weight to 0.15% by weight.

2. The method of claim 1, wherein the formulation comprises ingenol-3-angelate (isoform `b`) in an amount from 0.01% by weight to 0.1% by weight.

3. The method of claim 1, wherein the ingenol-3-angelate (isoform `b`) has a rate of permeation across the skin between 11 ng cm.sup.-2 h.sup.-1 and 1 .mu.g cm.sup.-2 h.sup.-1.

4. The method of claim 1, wherein the amount of ingenol-3-angelate (isoform `b`) applied to the skin is between 0.01 .mu.g cm.sup.-2 and 1 mg cm.sup.-2.

5. The method of claim 1, wherein the amount of ingenol-3-angelate (isoform `b`) applied to the skin is between 0.01 .mu.g cm.sup.-2 and 100 .mu.g cm.sup.-2.

6. The method of claim 1, wherein the acidifying agent is an acid buffer.

7. The method of claim 6, wherein the acid buffer is selected from the group consisting of a citrate buffer, a phosphate buffer, an acetate buffer, and a citrate-phosphate buffer.

8. The method of claim 7, wherein the acid buffer is a citrate buffer.

9. The method of claim 7, wherein the formulation comprises from 0.5% by weight to 10% by weight acid buffer.

10. The method of claim 1, wherein the formulation further comprises a pharmaceutically acceptable solvent, wherein the solvent is selected from the group consisting of polyethylene glycol, methyl ethyl ketone, ethyl acetate, diethyl ether, and benzyl alcohol.

11. The method of claim 10, wherein the solvent is benzyl alcohol.

12. The method of claim 11, wherein the formulation comprises 0.9% by weight benzyl alcohol.

13. The method of claim 1, wherein the formulation further comprises a penetration enhancer, wherein the penetration enhancer is selected from the group consisting of isopropyl alcohol, a sulphoxide, an azone, a pyrrolidone, and an alkanol.

14. The method of claim 13, wherein the penetration enhancer is isopropyl alcohol.

15. The method of claim 14, wherein the formulation comprises 30% by weight isopropyl alcohol.

16. The method of claim 1, wherein the formulation further comprises a gelling agent.

17. The method of claim 16, wherein the gelling agent is selected from the group consisting of a hydroxyalkyl cellulose polymer, carboxymethyl cellulose, methylhydroxyethyl cellulose, methyl cellulose, a carbomer, and a carrageenan.

18. The method of claim 17, wherein the gelling agent is hydroxyethylcellulose.

19. The method of claim 18, wherein the formulation comprises 1.5% by weight hydroxyethylcellulose.

20. The method of claim 17, wherein the formulation comprises from 1% by weight to 5% by weight gelling agent.

21. The method of claim 1, wherein the formulation has a pH of no greater than 4.5.

22. The method of claim 1, wherein the formulation has a pH of no less than 2.5.

23. The method of claim 1, wherein ingenol-3-angelate (isoform `b`) is the only active ingredient in the formulation.

24. The method of claim 1, wherein the formulation is selected from the group consisting of a gel, a cream, an ointment, a paint, a lotion, and a foam.

25. The method of claim 1, wherein the formulation is sterilized.

26. The method of claim 1, wherein the formulation is suitable for storage at 2-8.degree. C.

27. The method of claim 1, wherein the formulation is suitable for storage at 2-8.degree. C. for at least one year.

28. A method of treating a condition in a subject in need thereof, the method comprising: topically administering a therapeutically effective amount of a pharmaceutical formulation comprising ingenol angelate and an acidifying agent to a skin lesion of the subject, at least about 95% of the ingenol angelate being ingenol-3-angelate (isoform `b`); wherein the pharmaceutical formulation comprises ingenol-3-angelate (isoform `b`) in an amount from 0.001% by weight to 0.15% by weight and the condition is selected from the group consisting of squamous cell carcinoma, basal cell carcinoma, malignant melanoma, and actinic keratosis.

29. The method of claim 28, wherein the condition is actinic keratosis.

30. The method of claim 28, wherein the formulation comprises ingenol-3-angelate (isoform `b`) in an amount from 0.01% by weight to 0.1% by weight.

31. The formulation of claim 1, wherein at least about 99% of the ingenol angelate is ingenol-3-angelate (isoform `b`).

32. The method of claim 28, wherein at least about 99% of the ingenol angelate is ingenol-3-angelate (isoform `b`).

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