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Last Updated: March 29, 2024

Claims for Patent: 8,895,557


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Summary for Patent: 8,895,557
Title:Pharmaceutical formulations of ecteinascidin compounds
Abstract: Ecteinascidin formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided.
Inventor(s): Beijnen; Jacob Hendrik (Amsterdam, NL), Nuijen; Bastiaan (Amsterdam, NL), Salve; Pilar Calvo (Madrid, ES), Barreira; Maria Tobio (Madrid, ES)
Assignee: Pharma Mar, S.A., Sociedad Unipersonal (Madrid, ES)
Application Number:11/261,876
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,895,557
Patent Claims: 1. A lyophilised anti-tumor composition comprising a single active anti-tumor compound and a disaccharide selected from sucrose, lactose and a combination thereof, wherein the anti-tumor compound is ET-743 and wherein the disaccharide is present in a sufficient amount to inhibit conversion of the ET-743 into ET-701, such that the ET-743 composition comprises less than 2% ET-701 after storage of the ET-743 composition at 5.degree. C. for 3 months.

2. The lyophilised anti-tumor composition according to claim 1, wherein said disaccharide is lactose.

3. The lyophilised anti-tumor composition according to claim 1, wherein said disaccharide is sucrose.

4. The lyophilised anti-tumor composition according to claim 1, wherein the ratio (w/w) of ET-743 to disaccharide is from about 1:100 to about 1:1500.

5. The lyophilised anti-tumor composition according to claim 4, wherein the ratio (w/w) of ET-743 to disaccharide is from about 1:250 to about 1:600.

6. The lyophilised anti-tumor composition according to claim 5, wherein the ratio (w/w) of ET-743 to disaccharide is about 1:400.

7. The lyophilised anti-tumor composition according to claim 1, which further comprises a buffering agent.

8. The lyophilised anti-tumor composition according to claim 7, wherein said buffering agent is selected from phosphate buffer, citrate buffer, glycine/hydrochloric acid buffer, and mixtures thereof.

9. The lyophilised anti-tumor composition according to claim 1, which further comprises a surface-active agent.

10. The lyophilised anti-tumor composition according to claim 9, wherein the surface-active agent is selected from polyoxyethylene 20 sorbitan monooleate, polyoxyl 40 stearate, and mixtures thereof.

11. The lyophilised anti-tumor composition according to claim 1, wherein the lyophilised formulation is in a vial.

12. The lyophilised anti-tumor composition according to claim 11, wherein ET-743 is present in an amount of about 250 micrograms.

13. The lyophilised anti-tumor composition according to claim 12, wherein said vial contains a composition comprising: about 0.25 mg ET-743, about 100 mg sucrose, and about 6.8 mg potassium dihydrogen phosphate.

14. The lyophilised anti-tumor composition according to claim 11, wherein ET-743 is present in an amount of about 1 mg.

15. The lyophilised anti-tumor composition according to claim 14, wherein said vial contains a formulation comprising: about 1.0 mg ET-743, about 400 mg sucrose, and about 27.2 mg potassium dihydrogen phosphate.

16. A method of making a lyophilised composition of ET-743 according to claim 1, comprising freeze-drying a bulk solution that comprises ET-743 and a disaccharide wherein said disaccharide is selected from sucrose, lactose and a combination thereof.

17. A method of reducing the formation of ET-701 in a composition of ET-743, comprising freeze-drying a bulk solution that comprises ET-743 and a disaccharide to yield a composition according to claim 1 wherein said disaccharide is selected from sucrose, lactose and a combination thereof.

18. A method of preparing a bulk solution for lyophilising to yield a composition according to claim 1, comprising dissolving ET-743 in an acidic medium, mixing the pre-dissolved ET-743 with other components of the bulk solution and, optionally, adjusting the pH of the final solution.

19. A method of preparing a solution for intravenous infusion, comprising: providing a vial that comprises a lyophilised ET-743 composition according to claim 1, adding water to form a reconstituted solution, and diluting said reconstituted solution with an aqueous system.

20. The lyophilised anti-tumor composition according to claim 3, further comprising a buffering agent.

21. The lyophilised anti-tumor composition according to claim 20, further comprising a surface-active agent.

22. A lyophilized anti-tumor composition comprising a single active anti-tumor compound and a disaccharide selected from sucrose, lactose and a combination thereof, wherein the anti-tumor compound is ET-743 and wherein the disaccharide is present in a sufficient amount to inhibit conversion of the ET-743 into ET-701, such that the ET-743 composition comprises less than 2% ET-701 after storage of the ET-743 composition at 25.degree. C. for 3 months.

23. The lyophilised anti-tumor composition according claim 22, wherein the lyophilised composition is in a vial.

24. The lyophilised anti-tumor composition according to claim 22, wherein the disaccharide is sucrose.

25. The lyophilised anti-tumor composition according to claim 22, wherein the disaccharide is lactose.

26. The lyophilised anti-tumor composition according to claim 22, further comprising a buffer.

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