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.

We claim: 
     
         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 1  or  2 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         4 . The method of  claim 1  or  2 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         5 . The method of  claim 1  or  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 6  or  7 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         9 . The method of  claim 6  or  7 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         10 . The method of  claim 6  or  7 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         11 . A method to induce remission or regression of 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. 
     
     
         12 . The method of  claim 11  to induce remission or regression of 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. 
     
     
         13 . The method of  claim 11  or  12 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         14 . The method of  claim 11  or  12 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         15 . The method of  claim 11  or  12 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         16 . A method to prevent 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. 
     
     
         17 . The method of  claim 16  to prevent 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. 
     
     
         18 . The method of  claim 16  or  17 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         19 . The method of  claim 16  or  17 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         20 . The method of  claim 16  or  17 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         21 . 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. 
     
     
         22 . The method of  claim 21  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. 
     
     
         23 . The method of  claim 21  or  22 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         24 . The method of  claim 21  or  22 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         25 . The method of  claim 21  or  22 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         26 . A method for treating chronic kidney disease, comprising administering an effective amount of tirzepatide or a pharmaceutically acceptable salt thereof, to a patient in need of such treatment. 
     
     
         27 . The method of  claim 26 , for treating chronic kidney disease 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. 
     
     
         28 . The method of  claim 26  for treating chronic kidney disease 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. 
     
     
         29 . The method of  claim 27  or  28 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         30 . The method of  claim 27  or  28 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         31 . The method of  claim 27  or  28 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         32 . A method for treating atherosclerosis, comprising administering an effective amount of tirzepatide or a pharmaceutically acceptable salt thereof, to a patient in need of such treatment. 
     
     
         33 . The method of  claim 32  for treating atherosclerosis 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. 
     
     
         34 . The method of  claim 32  for treating atherosclerosis 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. 
     
     
         35 . The method of  claim 33  or  34 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         36 . The method of  claim 33  or  34 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         37 . The method of  claim 33  or  34 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         38 . A method for treating nonalcohol fatty liver disease, comprising: administering an effective amount of tirzepatide or a pharmaceutically acceptable salt thereof to a patient in need of such treatment. 
     
     
         39 . The method of  claim 38  for treating nonalcohol fatty liver disease, 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. 
     
     
         40 . The method of  claim 38  for treating nonalcohol fatty liver disease, 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. 
     
     
         41 . The method of  claim 39  or  40 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         42 . The method of  claim 39  or  40 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         43 . The method of  claim 39  or  40 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         44 . A method for treating nonalcohol steatohepatitis, comprising: administering an effective amount of tirzepatide or a pharmaceutically acceptable salt thereof to a patient in need of such treatment. 
     
     
         45 . The method of  claim 44  for treating nonalcohol steatohepatitis, 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. 
     
     
         46 . The method of  claim 44  for treating nonalcohol steatohepatitis, 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. 
     
     
         47 . The method of  claim 45  or  46 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         48 . The method of  claim 45  or  46 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         49 . The method of  claim 45  or  46 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         50 . 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. 
     
     
         51 . The method of  claim 50  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. 
     
     
         52 . The method of  claim 50  or  51 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         53 . The method of  claim 50  or  51 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         54 . The method of  claim 50  or  51 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg. 
     
     
         55 . A method for treating diabetic kidney disease, 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. 
     
     
         56 . The method of  claim 55  for treating diabetic kidney disease, 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. 
     
     
         57 . The method of  claim 55  or  56 , wherein the escalation dose is about 2.5 mg and the maintenance dose is about 5.0 mg. 
     
     
         58 . The method of  claim 55  or  56 , wherein the escalation dose is about 7.5 mg and the maintenance dose is about 10.0 mg. 
     
     
         59 . The method of  claim 55  or  56 , wherein the escalation dose is about 12.5 mg and the maintenance dose is about 15.0 mg.