US2016067184A1PendingUtilityA1

Oral Dosing of GLP-1 Compounds

Assignee: NOVO NORDISK ASPriority: May 2, 2013Filed: May 2, 2014Published: Mar 10, 2016
Est. expiryMay 2, 2033(~6.8 yrs left)· nominal 20-yr term from priority
A61K 38/26A61K 9/2054A61P 3/04A61K 31/166A61K 9/20A61K 9/2013A61P 3/10A61K 9/0053A61P 43/00
70
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Claims

Abstract

The present invention relates to improved uses of GLP-1 peptides in oral therapy.

Claims

exact text as granted — not AI-modified
1 . A solid composition comprising a GLP-1 peptide and an enhancer,
 wherein   a) said peptide has a plasma half-life in humans of at least 60 hours;   b) said composition is administered orally at least 3 times; and   c) said composition is administered such that the ratio between the plasma half-life in days in humans of said peptide and the dosing interval in days of said composition is more than 2:1.   
     
     
         2 . The composition according to  claim 1 , wherein said composition is administered every second day or more frequently. 
     
     
         3 . The composition according to  claim 2 , wherein said composition is administered once daily. 
     
     
         4 . The composition according to  claim 1 , wherein said composition is in the form of a tablet. 
     
     
         5 . The composition according to  claim 1 , wherein said composition is administered at least 5 times. 
     
     
         6 . The composition according to  claim 1 , wherein said enhancer is a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, such as SNAC. 
     
     
         7 . The composition according to  claim 6 , wherein the amount of SNAC is 100-500 mg SNAC. 
     
     
         8 . The composition according to  claim 1 , wherein said enhancer is a salt of capric acid, such as sodium caprate. 
     
     
         9 . The composition according to  claim 1 , wherein said peptide has plasma half-life in humans of at least 72 hours. 
     
     
         10 . The composition according to  claim 1 , wherein said peptide is administered in an amount of 0.01-100 mg. 
     
     
         11 . The composition according to  claim 7 , wherein said composition comprises 1-100 mg GLP-1 peptide. 
     
     
         12 . The composition according to  claim 11 , wherein said peptide is semaglutide or N ε26 {2-[2-(2-{2-[2-(2-{(S)-4-Carboxy-4-[10-(4-carboxy-phenoxy)decanoylamino]butyrylamino}ethoxy)ethoxy]acetylamino}ethoxy)ethoxy]acetyl}, N ε37 -{2-[2-(2-{2-[2-(2-{(S)-4-carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butyrylamino}ethoxy)-ethoxy]acetylamino}ethoxy)ethoxy]acetyl}-[Aib 8 ,Arg 34 ,Lys 37 ]GLP-1(7-37)-OH. 
     
     
         13 . The composition according to  claim 12 , wherein said composition comprises 2-60 mg semaglutide and 200-400 mg SNAC. 
     
     
         14 . The composition according to  claim 1 , wherein said composition further comprises one or more pharmaceutically acceptable excipients. 
     
     
         15 . (canceled) 
     
     
         16 . A method for treating diabetes and/or obesity in a subject in need of such treatment, said method comprising administering to said subject a therapeutically effective amount of a composition according to  claim 1 . 
     
     
         17 . The composition according to  claim 6 , wherein the amount of SNAC is 50-90%(w/w) of said composition. 
     
     
         18 . The composition according to  claim 17 , wherein said composition comprises 1-100 mg GLP-1 peptide. 
     
     
         19 . The composition according to  claim 18 , wherein said peptide is semaglutide or N ε26 {2-[2-(2-{2-[2-(2-{(S)-4-Carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butyrylamino}ethoxy)-ethoxy]acetylamino}ethoxy)ethoxy]acetyl}, N ε37 -{2-[2-(2-{2-[2-(2-{(S)-4-carboxy-4-[10-(4-carboxyphenoxy)decanoylamino]butyrylamino}ethoxy)ethoxy]acetylamino}ethoxy)ethoxy]acetyl}-[Aib 8 ,Arg 34 ,Lys 37 ]GLP-1(7-37)-OH. 
     
     
         20 . The composition according to  claim 19 , wherein said composition comprises 2-60 mg semaglutide.

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