Claims for Patent: 12,343,382

Summary for Patent: 12,343,382

Title:	Methods of using a GIP/GLP1 co-agonist for therapy
Abstract:	The present invention provides a method for increasing glycemic control in a patient in need thereof, by administering tirzepatide, or a pharmaceutically acceptable salt thereof. The present invention provides a method for improving weight management in a patient in need thereof, by administering tirzepatide, or a pharmaceutically acceptable salt thereof. Further providing a method for treating a condition selected from atherosclerosis, chronic kidney disease, NAFLD, and NASH. Further provided is a method to prevent or induce remission of diabetes comprising administration of tirzepatide, or a pharmaceutically acceptable salt thereof. Further provided is a dosing regimen for increasing glycemic control, improving weight management, and/or treating dyslipidemia.
Inventor(s):	Charles T. BENSON, Axel Haupt, Melissa Kay THOMAS, Shweta URVA
Assignee:	Eli Lilly and Co
Application Number:	US17/366,453
Patent Claims:	1. A method of treating type 2 diabetes in a patient in need thereof, comprising: administering an escalation dose about once weekly for a minimum of at least about two weeks and thereafter administering a maintenance dose about once weekly for a minimum of at least about two weeks; wherein the escalation dose is selected from the group consisting of about 2.5 mg, about 7.5 mg and about 12.5 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; and wherein the maintenance dose is selected from the group consisting of about 5.0 mg, about 10.0 mg and about 15.0 mg of tirzepatide, or a pharmaceutically acceptable salt thereof. 2. The method of claim 1 for treating type 2 diabetes in a patient in need thereof, comprising: administering at least one escalation dose about once weekly for a minimum of about four weeks and at least one maintenance dose about once weekly for a minimum of about four weeks following the escalation dose; wherein the escalation dose is selected from the group consisting of about 2.5 mg, about 7.5 mg and about 12.5 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; wherein the maintenance dose is selected from the group consisting of about 5.0 mg, about 10.0 mg and about 15.0 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; and wherein the maintenance dose following an escalation dose is a 2.5 mg increment. 3. The method of claim 2, wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 4. The method of claim 2, wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 5. The method of claim 2, wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 6. A method of improving glycemic control in a patient in need thereof, comprising: administering an escalation dose about once weekly for a minimum of at least about two weeks and thereafter administering a maintenance dose about once weekly for a minimum of at least about two weeks; wherein the escalation dose is selected from the group consisting of about 2.5 mg, about 7.5 mg and about 12.5 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; and wherein the maintenance dose is selected from the group consisting of about 5.0 mg, about 10.0 mg and about 15.0 mg of tirzepatide, or a pharmaceutically acceptable salt thereof. 7. The method of claim 6 of improving glycemic control in a patient in need thereof, comprising: administering an escalation dose about once weekly for a minimum of about four weeks and thereafter administering a maintenance dose about once weekly for a minimum of about four weeks; wherein the escalation dose is selected from the group consisting of about 2.5 mg, about 7.5 mg and about 12.5 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; wherein the maintenance dose is selected from the group consisting of about 5.0 mg, about 10.0 mg and about 15.0 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; and wherein the maintenance dose following an escalation dose is about a 2.5 mg incremental increase relative to that escalation dose. 8. The method of claim 7, wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 9. The method of claim 7, wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 10. The method of claim 7, wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 11. A method to improve weight management, in a patient in need thereof, comprising: administering an escalation dose about once weekly for a minimum of at least about two weeks and thereafter administering a maintenance dose about once weekly for a minimum of at least about two weeks; wherein the escalation dose is selected from the group consisting of about 2.5 mg, about 7.5 mg and about 12.5 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; and wherein the maintenance dose is selected from the group consisting of about 5.0 mg, about 10.0 mg and about 15.0 mg of tirzepatide, or a pharmaceutically acceptable salt thereof. 12. The method of claim 11 to improve weight management, in a patient in need thereof, comprising: administering at least one escalation dose about once weekly for a minimum of about four weeks and at least one maintenance dose about once weekly for a minimum of about four weeks following the escalation dose; wherein the escalation dose is selected from the group consisting of about 2.5 mg, about 7.5 mg and about 12.5 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; wherein the maintenance dose is selected from the group consisting of about 5.0 mg, about 10.0 mg and about 15.0 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; and wherein the maintenance dose following an escalation dose is a 2.5 mg increment. 13. The method of claim 12, wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 14. The method of claim 12, wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 15. The method of claim 12, wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 16. A method for treating obesity, in a patient in need thereof, comprising: administering an escalation dose about once weekly for a minimum of at least about two weeks and thereafter administering a maintenance dose about once weekly for a minimum of at least about two weeks; wherein the escalation dose is selected from the group consisting of about 2.5 mg, about 7.5 mg and about 12.5 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; and wherein the maintenance dose is selected from the group consisting of about 5.0 mg, about 10.0 mg and about 15.0 mg of tirzepatide, or a pharmaceutically acceptable salt thereof. 17. The method of claim 16 for treating obesity, in a patient in need thereof, comprising: administering at least one escalation dose about once weekly for a minimum of about four weeks and at least one maintenance dose about once weekly for a minimum of about four weeks following the escalation dose; wherein the escalation dose is selected from the group consisting of about 2.5 mg, about 7.5 mg and about 12.5 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; wherein the maintenance dose is selected from the group consisting of about 5.0 mg, about 10.0 mg and about 15.0 mg of tirzepatide, or a pharmaceutically acceptable salt thereof; and wherein the maintenance dose following an escalation dose is a 2.5 mg increment. 18. The method of claim 17, wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 19. The method of claim 17, wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 20. The method of claim 17, wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 21. A method for improving glycemic control in a patient comprising administering to the patient tirzepatide in once weekly doses, the administering comprising: administering a first once weekly dose of 2.5 mg for four weeks; increasing the once weekly dose by increments of 2.5 mg to a once weekly maintenance dose of 5, 10 or 15 mg, where each increased once weekly dose is administered for at least four weeks; and administering the maintenance dose of 5, 10, or 15 mg once weekly to improve the glycemic control in the patient. 22. The method of claim 21, wherein the patient has type 2 diabetes. 23. The method of claim 21, wherein the improved glycemic control comprises reducing the patient's level of HbA1c below 7%. 24. The method of claim 21, wherein the improved glycemic control comprises reducing the patient's level of HbA1c below 5.7%. 25. The method of claim 21, wherein the improved glycemic control reduces the patient's body weight by at least 5%. 26. The method of claim 21, wherein the improved glycemic control reduces the patient's body weight by at least 10%. 27. The method of claim 21, further comprising administering metformin to the patient. 28. The method of claim 21, wherein the maintenance dose is 5 mg. 29. The method of claim 21, wherein the maintenance dose is 10 mg. 30. The method of claim 21, wherein the maintenance dose is 15 mg. 31. The method of claim 30, further comprising reducing the maintenance dose to 10 mg. 32. The method of claim 21, wherein the administering the maintenance dose once weekly provides greater improved glycemic control and a reduced risk of nausea, vomiting, and diarrhea compared to treatment with 1.5 mg of dulaglutide once weekly. 33. The method of claim 21, wherein the administering the maintenance dose once weekly provides a less than a 31% of a risk experiencing a Previously Presented event of nausea, vomiting, and diarrhea on a weekly basis. 34. The method of claim 21, wherein the administering the maintenance dose once weekly provides not more than a 22% of a risk experiencing a Previously Presented event of nausea, vomiting, and diarrhea on a weekly basis. 35. The method of claim 21, wherein the tirzepatide is administered subcutaneously to the patient. 36. The method of claim 21, wherein the tirzepatide is administered as a 1 ml aqueous solution. 37. The method of claim 21, wherein the tirzepatide is administered as a pharmaceutically acceptable salt of tirzepatide. 38. The method of claim 22 wherein the tirzepatide is administered subcutaneously to the patient. 39. A method for improving glycemic control in a patient comprising administering to the patient tirzepatide in once-weekly doses, the administering comprising; administering a first once-weekly dose of 2.5 mg for four weeks; increasing the once-weekly dose by increments of 2.5 mg to a once weekly maintenance dose of 5, 10, or 15 mg, wherein each increased once weekly dose is administered for at least four weeks; and administering the maintenance dose of 5, 10, or 15 mg once weekly to improve glycemic control in the patient, wherein the patient has type 2 diabetes and the tirzepatide is administered subcutaneously to the patient. 40. The method of claim 39, wherein the improved glycemic control comprises reducing the patient's level of HbA1c below 7%. 41. The method of claim 39, wherein the improved glycemic control comprises reducing the patient's level of HbA1c below 5.7%. 42. The method of claim 39, wherein the improved glycemic control reduces the patient's body weight by at least 5%. 43. The method of claim 39, wherein the improved glycemic control reduces the patient's body weight by at least 10%. 44. The method of claim 39, further comprising administering metformin to the patient. 45. The method of claim 39, wherein the maintenance dose is 5 mg. 46. The method of claim 39, wherein the maintenance dose is 10 mg. 47. The method of claim 39, wherein the maintenance dose is 15 mg. 48. The method of claim 47, further comprising reducing the maintenance dose to 10 mg. 49. The method of claim 39, wherein the administering the maintenance dose once weekly provides greater improved glycemic control and a reduced risk of nausea, vomiting, and diarrhea compared to treatment with 1.5 mg of dulaglutide once weekly. 50. The method of claim 39, wherein the administering the maintenance dose once weekly provides a less than a 31% of a risk experiencing a Previously Presented event selected from the group consisting of nausea, vomiting, and diarrhea, on a weekly basis. 51. The method of claim 39, wherein the administering the maintenance dose once weekly provides not more than a 22% of a risk experiencing a new event selected from the group consisting of nausea, vomiting, and diarrhea, on a weekly basis.