US2022105035A1PendingUtilityA1

Amorphous solid dispersions of dasatinib and uses thereof

79
Assignee: NANOCOPOEIA LLCPriority: Jan 24, 2020Filed: Dec 15, 2021Published: Apr 7, 2022
Est. expiryJan 24, 2040(~13.5 yrs left)· nominal 20-yr term from priority
Inventors:Christian F. WertzTzehaw Chen
A61K 31/4439A61K 45/06A61K 9/10A61K 31/4164A61K 31/426A61K 9/2077A61K 2300/00A61K 47/14A61K 31/341A61K 31/506A61P 35/02A61K 47/32A61K 9/146A61K 9/0053A61K 47/38
79
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Claims

Abstract

Amorphous solid dispersions and pharmaceutical compositions of the protein kinase inhibitor dasatinib. The pharmaceutical compositions may be used in methods of treating a proliferative disorder such as cancer, or in methods of delivering dasatinib to patients without regard to whether the patient is concurrently administered a gastric acid-reducing agent, or without regard to whether the patient has an elevated gastric pH. The compositions may be particularly suitable for patients afflicted by achlorhydria or hypochlorhydria, or Helicobacter pylori infection.

Claims

exact text as granted — not AI-modified
1 - 43 . (canceled) 
     
     
         44 . A method of treating a proliferative disorder in a patient in need thereof, the method comprising administering to the patient a pharmaceutical composition comprising an amorphous solid dispersion;
 wherein the amorphous solid dispersion consists essentially of dasatinib, a polymer or copolymer of N-vinylpyrrolidone, and optionally one or more functional components selected from the group consisting of antioxidants, wetting agents, and solubilizers;   wherein the dasatinib and the one or more polymers are present in the amorphous solid dispersion in a w/w ratio of 30:70 to 95:5 (dasatinib:polymer); and   wherein the patient has elevated gastric pH.   
     
     
         45 . The method of  claim 44 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a polyvinylpyrrolidone. 
     
     
         46 . The method of  claim 44 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a vinylpyrrolidone/vinyl acetate copolymer. 
     
     
         47 . The method of  claim 44 , wherein the amorphous solid dispersion includes one or more functional components selected from the group consisting of antioxidants, wetting agents, and solubilizers. 
     
     
         48 . The method of  claim 47 , wherein the amorphous solid dispersion includes one or more solubilizers. 
     
     
         49 . The method of  claim 48 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. 
     
     
         50 . The method of  claim 44 , wherein the pharmaceutical composition comprises the amorphous solid dispersion and one or more pharmaceutically acceptable additives. 
     
     
         51 . The method of  claim 50 , wherein the one or more pharmaceutically acceptable additives includes one or more solubilizers. 
     
     
         52 . The method of  claim 51 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. 
     
     
         53 . The method of  claim 44 , wherein the pharmaceutical composition is a gastric acid-insensitive composition. 
     
     
         54 . A method of treating a proliferative disorder in a patient in need thereof and having elevated gastric pH, the method comprising:
 (a) identifying a condition by which the patient's gastric pH is chronically elevated; and   (b) administering to the patient a therapeutically effective amount of a pharmaceutical composition comprising an amorphous solid dispersion;   wherein the amorphous solid dispersion consists essentially of dasatinib, a polymer or copolymer of N-vinylpyrrolidone, and optionally one or more functional components selected from the group consisting of antioxidants, wetting agents, and solubilizers;   wherein the dasatinib and the one or more polymers are present in the amorphous solid dispersion in a w/w ratio of 30:70 to 95:5 (dasatinib:copolymer); and   wherein the therapeutically effective amount comprises 20 mg to 140 mg dasatinib.   
     
     
         55 . The method of  claim 54 , wherein the condition is achlorhydria or hypochlorhydria. 
     
     
         56 . The method of  claim 54 , wherein the condition is infection by  Helicobacter pylori.    
     
     
         57 . The method of  claim 54 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a polyvinylpyrrolidone. 
     
     
         58 . The method of  claim 54 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a vinylpyrrolidone/vinyl acetate copolymer. 
     
     
         59 . The method of  claim 54 , wherein the amorphous solid dispersion includes one or more functional components selected from the group consisting of antioxidants, wetting agents, and solubilizers. 
     
     
         60 . The method of  claim 54 , wherein the amorphous solid dispersion includes one or more solubilizers. 
     
     
         61 . The method of  claim 60 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. 
     
     
         62 . The method of  claim 54 , wherein the pharmaceutical composition comprises the amorphous solid dispersion and one or more pharmaceutically acceptable additives. 
     
     
         63 . The method of  claim 62 , wherein the one or more pharmaceutically acceptable additives includes one or more solubilizers. 
     
     
         64 . The method of  claim 63 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. 
     
     
         65 . The method of  claim 54 , wherein the pharmaceutical composition is a gastric acid-insensitive composition. 
     
     
         66 . A method of delivering a therapeutically relevant exposure of dasatinib to a subject who has elevated gastric pH, the method comprising administering to the subject a pharmaceutical composition comprising an amorphous solid dispersion;
 wherein the amorphous solid dispersion consists essentially of dasatinib, a polymer or copolymer of N-vinylpyrrolidone, and optionally one or more functional components selected from the group consisting of antioxidants, wetting agents, and solubilizers; and   wherein the dasatinib and the one or more polymers are present in the amorphous solid dispersion in a w/w ratio of 30:70 to 95:5 (dasatinib:copolymer).   
     
     
         67 . The method of  claim 66 , wherein the subject is a human patient. 
     
     
         68 . The method of  claim 66 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a polyvinylpyrrolidone. 
     
     
         69 . The method of  claim 66 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a vinylpyrrolidone/vinyl acetate copolymer. 
     
     
         70 . The method of  claim 66 , wherein the amorphous solid dispersion includes one or more solubilizers. 
     
     
         71 . The method of  claim 70 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer. 
     
     
         72 . The method of  claim 66 , wherein the pharmaceutical composition comprises the amorphous solid dispersion and one or more pharmaceutically acceptable additives. 
     
     
         73 . The method of  claim 72 , wherein the one or more pharmaceutically acceptable additives includes polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer.

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