IP Library › Granted Patent US 12,558,355
Granted Patent B2
US 12,558,355 · App. 18/137,722 · Granted Feb 24, 2026

Amorphous solid dispersions of dasatinib and uses thereof

Inventors: Christian F. Wertz (Saint Louis Park, MN); Tzehaw Chen (Corcoran, MN)
Assignee: Handa Therapeutics, LLC
A61K31/506A61K9/0053A61K9/10A61K31/341A61K31/4164A61K31/426A61K31/4439A61K47/14A61K47/32A61K47/38
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Quick Facts
Patent No.
US 12,558,355
App. No.
18/137,722
Granted
Feb 24, 2026
Kind
B2
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 (32)

1 . 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 polymer or copolymer of N-vinylpyrrolidone are present in the amorphous solid dispersion in a w/w ratio of 30:70 to 95:5 (dasatinib:polymer); and

wherein the therapeutically effective amount comprises 20 mg to 140 mg dasatinib.

2 . The method of claim 1 , wherein the condition is achlorhydria or hypochlorhydria.

3 . The method of claim 1 , wherein the condition is infection by Helicobacter pylori.

4 . The method of claim 1 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a polyvinylpyrrolidone.

5 . The method of claim 1 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a vinylpyrrolidone/vinyl acetate copolymer.

6 . The method of claim 1 , wherein the amorphous solid dispersion includes one or more functional components selected from the group consisting of antioxidants, wetting agents, and solubilizers.

7 . The method of claim 1 , wherein the amorphous solid dispersion includes one or more solubilizers.

8 . The method of claim 7 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer.

9 . The method of claim 1 , wherein the pharmaceutical composition comprises the amorphous solid dispersion and one or more pharmaceutically acceptable additives.

10 . The method of claim 9 , wherein the one or more pharmaceutically acceptable additives includes one or more solubilizers.

11 . The method of claim 10 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer.

12 . 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 polymer or copolymer of N-vinylpyrrolidone 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.

13 . The method of claim 12 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a polyvinylpyrrolidone.

14 . The method of claim 12 , wherein the polymer or copolymer of N-vinylpyrrolidone includes a vinylpyrrolidone/vinyl acetate copolymer.

15 . The method of claim 12 , wherein the amorphous solid dispersion includes one or more functional components selected from the group consisting of antioxidants, wetting agents, and solubilizers.

16 . The method of claim 15 , wherein the amorphous solid dispersion includes one or more solubilizers.

17 . The method of claim 16 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer.

18 . The method of claim 12 , wherein the pharmaceutical composition comprises the amorphous solid dispersion and one or more pharmaceutically acceptable additives.

19 . The method of claim 18 , wherein the one or more pharmaceutically acceptable additives includes one or more solubilizers.

20 . The method of claim 19 , wherein the one or more solubilizers comprises polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer.

21 . 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 copolymer are present in the amorphous solid dispersion in a w/w ratio of 30:70 to 95:5 (dasatinib:copolymer).

22 . The method of claim 21 , wherein the subject is a human patient.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 28, 2025
From: PXMMI, LLC
To: HANDA THERAPEUTICS, LLC
Reel/Frame 071084/0182 →
NUNC PRO TUNC ASSIGNMENT Recorded Apr 24, 2025
From: NANOCOPOEIA, LLC
To: PXMMI, LLC
Reel/Frame 070939/0374 →
AFFIDAVIT RE: ASSGNMENT FOR THE BENEFIT OF CREDITORS (MINNESOTA STATE COURT FILE NO. 62-CV-24-5879) Recorded Mar 11, 2025
From: NANOCOPOEIA, LLC
To: LIGHTHOUSE MANAGEMENT GROUP, INC.
Reel/Frame 070733/0519 →
AFFIDAVIT RE: ASSGNMENT FOR THE BENEFIT OF CREDITORS (MINNESOTA STATE COURT FILE NO. 62-CV-24-5879) Recorded Mar 11, 2025
From: LIGHTHOUSE MANAGEMENT GROUP, INC.
To: NANOCOPOEIA, LLC
Reel/Frame 070908/0001 →
Continuity (6)
Continuation 17888060 · Aug 15, 2022
Continuation 17549104 · Dec 13, 2021
Continuation PCTUS2021014742 · Jan 22, 2021
Provisional Application 63018182 · Apr 30, 2020
Provisional Application 62965650 · Jan 24, 2020
Related Publication 20230355620A1 · Nov 9, 2023
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