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Last Updated: March 28, 2024

Claims for Patent: 6,455,518


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Summary for Patent: 6,455,518
Title: Pharmaceutical compositions for the treatment of transplant rejection, autoimmune or inflammatory conditions comprising cyclosporin a and 40-O-(2-hydroxyethyl)-rapamycin
Abstract:A synergistic combination of an IL-2 transcription inhibitor (e.g., cyclosporin A or FK506) and 40-O-(2-hydroxyethyl)-rapamycin is provided, which is useful in the treatment and prevention of transplant rejection and also certain autoimmune and inflammatory diseases, together with novel pharmaceutical compositions comprising an IL-2 transcription inhibitor in combination with a rapamycin, e.g., 40-O-(2-hydroxyethyl)-rapamycin.
Inventor(s): Zenke; Gerhard (Rheinfelden, DE), Schuurman; Hendrik (Basel, CH), Haeberlin; Barbara (Riehen, CH), Meinzer; Armin (Buggingen, DE)
Assignee: Novartis AG (Basel, CH)
Application Number:09/758,301
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,455,518
Patent Claims: 1. An IL-2 transcription inhibitor and 40-O-(2-hydroxyethyl)-rapamycin as a combined pharamceutical preparation in the weight ratio 2:1 to 180:1 for simultaneous, separate, or sequential use in synergistically effective amounts.

2. A pharmaceutical composition comprising (I) an IL-2 transcription inhibitor and (II) 40-O-(2-hydroxyethyl)-rapamycin, wherein the weight ratio II is 2:1 to 180:1, in combination or association with a pharmaceutically acceptable diluent or carrier.

3. A composition of claim 2 in the form of a microemulsion or a microemulsion preconcentrate or a solid dispersion.

4. A composition of claim 3 which is a microemulsion preconcentrate formulation.

5. A composition of claim 3 which is a solid dispersion formulation.

6. A composition of claim 2 wherein I and II are present in an oil-in-water microemulsion preconcentrate comprising a hydrophilic phase, a lipophilic phase, and a surfactant.

7. A method of treating or preventing an autoimmune or inflammatory condition or transplant rejection in a subject suffering from or at risk for such condition or rejection, comprising co-administering synergistically effective amounts of (I) an IL-2 transcription inhibitor and (II) 40-O-(2-hydroxyethyl)-rapamycin in the weight ratio 2:1 to 180:1.

8. The method of claim 7 wherein the ratio is 5:1 to 60:1.

9. The method of claim 8 wherein the ratio is 10:1 to 20:1.

10. The method of claim 9 wherein the ratio is 16:1.

11. A method of treating or preventing chronic rejection of a heart, lung, or kidney transplant in a subject suffering from or at risk for such rejection, comprising co-administering together or at substantially the same time synergistically effective amounts of (I) an IL-2 transcription inhibitor and (II) 40-O-(2-hydroxyethyl)-rapamycin.

12. The method of claim 11 wherein the compounds are administered as a fixed combination.

13. The method of claim 11 wherein the weight ratio II is 5:1 to 50:1.

14. The method of claim 11 wherein the weight ratio is 10:1 to 20:1.

15. The method of claim 11 wherein the weight ratio is 16:1.

16. The method of claim 11 wherein compounds I and II are co-administered in combination or association with a pharmaceutically acceptable diluent or carrier.

17. The method of claim 16 wherein compounds I and II are co-administered in the form of a microemulsion, a microemulsion preconcentrate, or a solid dispersion.

18. A kit comprising (I) an IL-2 transcription inhibitor and (II) 40-O-(2-hydroxyethyl)-rapamycin in separate unit dosage forms, wherein said unit dosage forms are suitable for administrating I and II in synergistically effective amounts, wherein the weight ratio II is 2:1 to 180:1.

19. The method of using an IL-2 transcription inhibitor in the manufacture of a pharmaceutical kit of claim 18.

20. The method of using 40-O-(2-hydroxyethyl)-rapamycin in the manufacture of a pharmaceutical kit of claim 18.

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