Claims for Patent: 7,713,947

Summary for Patent: 7,713,947

Title:	Cladribine regimen for treating multiple sclerosis
Abstract:	The present invention is related to the use of Cladribine for the preparation of a pharmaceutical formulation for the treatment of multiple sclerosis, especially relapsing-remitting multiple sclerosis or early secondary progressive multiple sclerosis, wherein the preparation is to be orally administered and wherein re-treatments are possible.
Inventor(s):	De Luca; Giampiero (Conches/Geneva, CH), Ythier; Arnaud (Collex-Bossy, CH), Munafo; Alain (Tartegnin, CH), Lopez-Bresnahan; Maria (Lincoln, MA)
Assignee:	Merck Serono S.A. (Coinsins, Vaud, CH)
Application Number:	11/722,018
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,713,947
Patent Claims:	1. A method of treating multiple sclerosis comprising the oral administration of a formulation comprising cladribine, wherein the formulation is to be orally administered following the sequential steps below: (i) an induction period wherein said cladribine formulation is administered and wherein the total dose of cladribine reached at the end of the induction period is from about 1.7 mg/kg to about 3.5 mg/kg; (ii) a cladribine-free period of between about 8 and about 10 months wherein no cladribine formulation is administered; (iii) a maintenance period wherein said cladribine formulation is administered and wherein the total dose of cladribine reached at the end of the maintenance period is lower than the total dose of cladribine reached at the end of the induction period (i); and (iv) a cladribine-free period wherein no cladribine formulation is administered. 2. The method according to claim 1, wherein the induction period lasts up to about 4 months. 3. The method according to claim 2, wherein the induction period lasts about 2 months. 4. The method according to claim 2, wherein the induction period lasts about 3 months. 5. The method according to claim 2, wherein the induction period lasts about 4 months. 6. The method according to claim 2, wherein the induction period lasts up to about 3 months. 7. The method according to claim 1, wherein the total dose of cladribine reached at the end of the induction period is about 1.7 mg/kg. 8. The method according to claim 1, wherein the total dose of cladribine reached at the end of the induction period is about 3.5 mg/kg. 9. The method according to claim 1, wherein the cladribine-free (iv) period lasts about 10 months. 10. The method according to claim 1, wherein the maintenance period lasts about 4 months. 11. The method according to claim 1, wherein the total dose of cladribine reached at the end of the maintenance period is about 1.7 mg/kg. 12. The method according to claim 1, wherein the formulation is to be orally administered following the sequential steps below: (i) an induction period wherein said cladribine formulation is orally administered and wherein the total dose of cladribine reached at the end of the induction period is from about 1.7 mg/kg to about 3.5 mg/kg; (ii) a cladribine-free period of between about 8 and about 10 months wherein no cladribine formulation is administered; (iii) a maintenance period wherein said cladribine formulation is administered and wherein the total dose of cladribine reached at the end of the maintenance period is lower than the total dose of cladribine reached at the end of the induction period (i); and (iv) a cladribine-free period wherein no cladribine formulation is administered; wherein the induction period lasts up to 4 months; the cladribine-free period (ii) lasts up to 10 months; the maintenance period (iii) lasts up to 2 months; the cladribine-free period (iv) lasts up to 10 months; the total dose of cladribine reached at the end of the maintenance period is about 1.7 mg/kg and steps (iii) to (iv) are repeated one, two or three times. 13. The method according to claim 12, wherein the total dose of cladribine reached at the end of the induction period is about 3.5 mg/kg and the total dose of cladribine reached at the end of the maintenance period is about 1.7 mg/kg. 14. The method according to claim 12, wherein the formulation is to be orally administered at a daily dose of 3 to 30 mg cladribine. 15. The method according to claim 14, wherein the formulation is to be orally administered at a daily dose of 10 mg cladribine. 16. The method according to claim 1, wherein the formulation is orally administered 1 to 7 days per month during the induction period. 17. The method according to claim 1, wherein the steps (iii) to (iv) are repeated at least one or two times. 18. The method according to claim 1, wherein said cladribine formulation is to be administered in combination with interferon-beta. 19. The method according to claim 12, wherein said cladribine formulation is to be administered in combination with interferon-beta. 20. A method of treating multiple sclerosis comprising the oral administration of a formulation comprising cladribine following the sequential steps below: (i) an induction period lasting from about 2 months to about 4 months wherein said formulation is orally administered and wherein the total dose of cladribine reached at the end of the induction period is from about 1.7 mg/kg to about 3.5 mg/kg; (ii) a cladribine-free period lasting from about 8 months to about 10 months, wherein no cladribine is administered; (iii) a maintenance period lasting from about 2 months to about 4 months, wherein said formulation is orally administered and wherein the total dose of cladribine reached at the end of the maintenance period is lower than the total dose of cladribine reached at the end of the induction period (i); (iv) a cladribine-free period wherein no cladribine is administered. 21. The method according to claim 20, wherein the induction period lasts about 4 months. 22. The method according to claim 20, wherein the induction period lasts about 2 months. 23. The method according to claim 20, wherein the total dose of cladribine reached at the end of the induction period is about 1.7 mg/kg. 24. The method according to claim 20, where the total dose of cladribine reached at the end of the induction period is about 3.5 mg/kg. 25. The method according to claim 20, wherein the cladribine-free period (ii) lasts about 10 months. 26. The method according to claim 20, wherein the cladribine-free (iv) period lasts 10 months. 27. The method according to claim 20, wherein the maintenance period lasts about 2 months. 28. The method according to claim 20, wherein the formulation is orally administered following the sequential steps below: (i) an induction period wherein said formulation is administered orally and wherein the total dose of cladribine reached at the end of the induction period is from about 1.7 mg/kg to about 3.5 mg/kg; (ii) a cladribine-free period wherein no cladribine is administered; (iii) a maintenance period wherein said formulation is administered orally and wherein the total dose of cladribine reached at the end of the maintenance period is lower than the total dose of cladribine reached at the end of the induction period (i); (iv) a cladribine-free period wherein no cladribine is administered; wherein the maintenance period (iii) lasts about 2 months; the cladribine-free period (iv) lasts about 10 months; the total dose of cladribine reached at the end of the maintenance period is about 1.7 mg/kg and steps (iii) to (iv) are repeatedly performed one, two or three times. 29. The method according to claim 20, wherein the total dose of cladribine reached at the end of the induction period is about 3.5 mg/kg and the total dose of cladribine reached at the end of the maintenance period is about 1.7 mg/kg. 30. The method according to claim 20, wherein the formulation is orally administered at a daily dose of 3 to 30 mg cladribine. 31. The method according to claim 20, wherein the formulation is orally administered at a daily dose of 10 mg cladribine. 32. The method according to claim 20, wherein the formulation is orally administered 1 to 7 days per month during the induction period. 33. The method according to claim 20, wherein the steps (iii) to (iv) are repeated at least one time. 34. The method according to claim 20, wherein the steps (iii) to (iv) are repeated at least two times. 35. The method according to claim 20, wherein the formulation is administered in combination with interferon-beta. 36. A method of treating multiple sclerosis comprising the oral administration of a formulation comprising cladribine following the sequential steps below: (i) an induction period lasting from about 2 months to about 4 months wherein said formulation is orally administered and wherein the total dose of cladribine reached at the end of the induction period is from about 1.7 mg/kg to about 3.5 mg/kg; (ii) a cladribine-free period lasting from about 8 months to about 10 months, wherein no cladribine is administered; (iii) a maintenance period lasting from about 2 months to about 4 months, wherein said formulation is orally administered and wherein the total dose of cladribine reached at the end of the maintenance period is about 1.7 mg/kg; (iv) a cladribine-free period wherein no cladribine is administered. 37. The method according to claim 36, wherein the induction period lasts about 4 months. 38. The method according to claim 36, wherein the induction period lasts about 2 months. 39. The method according to claim 36, wherein the total dose of cladribine reached at the end of the induction period is about 1.7 mg/kg. 40. The method according to claim 36, where the total dose of cladribine reached at the end of the induction period is about 3.5 mg/kg. 41. The method according to claim 36, wherein the cladribine-free period (ii) lasts about 10 months. 42. The method according to claim 36, wherein the cladribine-free (iv) period lasts 10 months. 43. The method according to claim 36, wherein the maintenance period lasts about 2 months. 44. The method according to claim 36, wherein the formulation is orally administered at a daily dose of 3 to 30 mg cladribine. 45. The method according to claim 36, wherein the formulation is orally administered at a daily dose of 10 mg cladribine. 46. The method according to claim 36, wherein the formulation is orally administered 1 to 7 days per month during the induction period. 47. The method according to claim 36, wherein the steps (iii) to (iv) are repeated at least one or two times. 48. The method according to claim 36, wherein the formulation is administered in combination with interferon-beta.