US2021260056A1PendingUtilityA1

Low-dose triple combination formulation

69
Assignee: THE GEORGE INST FOR GLOBAL HEALTHPriority: Mar 25, 2019Filed: May 11, 2021Published: Aug 26, 2021
Est. expiryMar 25, 2039(~12.7 yrs left)· nominal 20-yr term from priority
Inventors:Stephen MacmahonAnthony Rodgers
A61P 13/12A61P 3/00A61P 3/04A61P 3/10A61K 31/4985A61K 31/351A61K 31/155A61K 45/06A61K 2300/00A61K 31/7048A61K 31/7034A61K 9/0053
69
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Claims

Abstract

Provided herein are pharmaceutical compositions that are useful for the treatment of diabetes and associated conditions, diseases, and disorders.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A pharmaceutical composition comprising:
 a) a dipeptidyl peptidase IV (DPP IV) inhibitor;   b) a biguanide; and   c) a subtype 2 sodium-glucose transport protein (SGLT2) inhibitor;   
       wherein (a), (b), and (c) are each at about 20-75% of the lowest diabetes therapeutic dose (LDTD). 
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the DPP IV inhibitor is sitagliptin, the biguanide is metformin, and the SGLT2 inhibitor is dapagliflozin or empagliflozin. 
     
     
         3 . The pharmaceutical composition of  claim 2 , wherein the dose of sitagliptin is from about 5.0 mg to about 18.75 mg, the dose of metformin is from about 100 mg to about 375 mg, and the dose of dapagliflozin is from about 1.0 mg to about 2.75 mg. 
     
     
         4 . The pharmaceutical composition of  claim 2 , wherein the dose of sitagliptin is from about 5.0 mg to about 18.75 mg, the dose of metformin is from about 100 mg to about 375 mg, and the dose of empagliflozin is from about 2.0 mg to about 7.5 mg. 
     
     
         5 . The pharmaceutical composition of  claim 1 , wherein:
 a) a dipeptidyl peptidase IV (DPP IV) inhibitor;   b) a biguanide; and   c) a subtype 2 sodium-glucose transport protein (SGLT2) inhibitor;   
       wherein (a) and (b) are each at about 65%-75% of the lowest diabetes therapeutic dose (LDTD) and (c) is at about 45%-55% of the lowest diabetes therapeutic dose (LDTD). 
     
     
         6 . The pharmaceutical composition of  claim 5 , wherein the DPP IV inhibitor is sitagliptin and the dose of sitagliptin is from about 16.25 mg to about 18.75 mg. 
     
     
         7 . The pharmaceutical composition of  claim 5 , wherein the biguanide is metformin and the dose of metformin is from about 325 mg to about 375 mg. 
     
     
         8 . The pharmaceutical composition of  claim 5 , wherein the SGLT2 inhibitor is dapagliflozin, and the dose of dapagliflozin from about 2.25 mg to about 2.75 mg. 
     
     
         9 . The pharmaceutical composition of  claim 5 , wherein the SGLT2 inhibitor is empagliflozin, and the dose of empagliflozin from about 4.5 mg to about 7.5 mg. 
     
     
         10 . The pharmaceutical composition of  claim 5 , wherein the DPP IV inhibitor is at about 70% of the lowest diabetes therapeutic dose (LDTD) for the DPP IV inhibitor. 
     
     
         11 . The pharmaceutical composition of  claim 5 , wherein the biguanide is at about 70% of the lowest diabetes therapeutic dose (LDTD) for the biguanide. 
     
     
         12 . The pharmaceutical composition of  claim 5 , wherein the SGLT2 inhibitor is at about 50% of the lowest diabetes therapeutic dose (LDTD) for the SGLT2 inhibitor. 
     
     
         13 . The pharmaceutical composition of  claim 5 , wherein the DPP IV inhibitor is sitagliptin, the biguanide is metformin, and the SGLT2 inhibitor is dapagliflozin or empagliflozin, 
     
     
         14 . The pharmaceutical composition of  claim 13 , wherein the dose of sitagliptin is about 17.5 mg, the dose of metformin is about 350 mg, and the dose of dapagliflozin is about 2.5 mg. 
     
     
         15 . The pharmaceutical composition of  claim 13 , wherein the dose of sitagliptin is about 17.5 mg, the dose of metformin is about 350 mg, and the dose of empagliflozin is about 5.0 mg. 
     
     
         16 . The pharmaceutical composition of  claim 5 , wherein the DPP IV inhibitor is sitagliptin and the dose of the sitagliptin is about 17.5 mg. 
     
     
         17 . The pharmaceutical composition of  claim 5 , wherein the biguanide is metformin and the dose of the metformin is about 350 mg. 
     
     
         18 . The pharmaceutical composition of  claim 5 , wherein the SGLT2 inhibitor is dapagliflozin and the dose of the dapagliflozin is about 2.5 mg. 
     
     
         19 . The pharmaceutical composition of  claim 5 , wherein the SGLT2 inhibitor is empagliflozin and the dose of the empagliflozin is about 5.0 mg. 
     
     
         20 . The pharmaceutical composition of  claim 1 , wherein (a), (b), and (c) are provided in one formulation. 
     
     
         21 . The pharmaceutical composition of  claim 1 , wherein (a), (b), and (c) are each provided in a separate formulation. 
     
     
         22 . The pharmaceutical composition of  claim 1 , wherein two of the (a), (b), and (c) are provided in one formulation. 
     
     
         23 . The pharmaceutical composition of  claim 1 , wherein the pharmaceutical composition is suitable for oral administration. 
     
     
         24 . The pharmaceutical composition of  claim 1 , wherein the pharmaceutical composition is in the form of pill, tablet, or capsule. 
     
     
         25 . The pharmaceutical composition of  claim 1 , wherein the metformin is formulated for immediate release. 
     
     
         26 . The pharmaceutical composition of  claim 1 , wherein the metformin is formulated for slow release. 
     
     
         27 . A method of treating diabetes in a subject in need thereof, comprising administering the pharmaceutical composition of  claim 1 . 
     
     
         28 . The method of  claim 27 , wherein the subject has persisting elevation of blood sugar after treatment with one or two of a DPP IV inhibitor, a biguanide, and an SGLT2 inhibitor at the LDTD or higher dose. 
     
     
         29 . The method of  claim 28 , wherein the administration of the pharmaceutical composition is an initial or first-line treatment of diabetes. 
     
     
         30 . A method of improving, slowing the progression of, or delaying a metabolic disorder such as diabetes mellitus, impaired glucose tolerance, impaired fasting blood glucose, hyperglycemia, postprandial hyperglycemia, overweight, obesity, metabolic syndrome, impaired renal function, gestational diabetes, new onset diabetes after transplantation (NODAT) and complications associated therewith, and post-transplant metabolic syndrome (PTMS) and complications associated therewith, comprising administering to a subject in need thereof the pharmaceutical composition of  claim 1 .

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