IP Library › Granted Patent US 12,465,606
Granted Patent B2
US 12,465,606 · App. 17/737,399 · Granted Nov 11, 2025

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 12,465,606
App. No.
17/737,399
Granted
Nov 11, 2025
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 (24)

1 . A pharmaceutical composition comprising an amorphous solid dispersion;

wherein the amorphous solid dispersion comprises dasatinib and a methacrylic acid and ethyl acrylate copolymer that exhibits pH-dependent solubility; 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).

2 . The pharmaceutical composition of claim 1 , wherein the copolymer is insoluble in an aqueous medium at pH of 5 or lower, and soluble in an aqueous medium at pH 5.5 or greater.

3 . The pharmaceutical composition of claim 1 , wherein the dasatinib and the copolymer are present in the amorphous solid dispersion in a w/w ratio of 40:60 to 70:30 (dasatinib: copolymer).

4 . The pharmaceutical composition of claim 3 , wherein the copolymer is insoluble in an aqueous medium at pH of 5 or lower, and soluble in an aqueous medium at pH 5.5 or greater.

5 . The pharmaceutical composition 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.

6 . The pharmaceutical composition of claim 5 , wherein the one or more functional components includes one or more antioxidants that are present in an amount of 0.001% to 2% by weight of the amorphous solid dispersion.

7 . The pharmaceutical composition of claim 6 , wherein the one or more antioxidants includes acetylcysteine, ascorbyl palmitate, butylated hydroxyanisole (“BHA”), butylated hydroxytoluene (“BHT”), monothioglycerol, potassium nitrate, sodium ascorbate, sodium formaldehyde sulfoxylate, sodium metabisulfite, sodium bisulfate, vitamin E or a derivative thereof, propyl gallate, ethylenediaminetetraacetic acid (“EDTA”) or a salt thereof, diethylenetriaminepentaacetic acid (“DTPA”), bismuth sodium triglycollamate, or a combination thereof.

8 . The pharmaceutical composition of claim 1 , comprising the amorphous solid dispersion and one or more pharmaceutically acceptable additives.

9 . The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is a solid dosage form suitable for oral administration.

10 . The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is a gastric acid-insensitive composition.

11 . A kit for sale to a user, the kit comprising a pharmaceutical composition and a package insert;

wherein the pharmaceutical composition comprises an amorphous solid dispersion, the amorphous solid dispersion comprising dasatinib and a methacrylic acid and ethyl acrylate copolymer that exhibits pH-dependent solubility; 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).

12 . The kit of claim 11 , wherein the package insert informs the user that the pharmaceutical composition can be co-administered with a gastric acid-reducing agent.

13 . The kit of claim 11 , wherein the package insert informs the user that the pharmaceutical composition can be co-administered with H2 antagonists or proton pump inhibitors.

14 . The kit of claim 11 , wherein the package insert does not comprise a warning that the pharmaceutical composition should not be co-administered with H2 antagonists or proton pump inhibitors.

15 . The kit of claim 11 , wherein the package insert informs the user that the pharmaceutical composition can be suitably administered if the user has chronically elevated gastric pH.

16 . The kit of claim 11 , wherein the package insert informs the user that the pharmaceutical composition can be suitably administered if the user has been diagnosed with or is afflicted by achlorhydria or hypochlorhydria.

17 . The kit of claim 11 , wherein the package insert informs the user that the pharmaceutical composition can be suitably administered if the user has been diagnosed with or is afflicted by Helicobacter pylori infection.

18 . The kit of claim 11 , wherein the copolymer is insoluble in an aqueous medium at pH of 5 or lower, and soluble in an aqueous medium at pH 5.5 or greater.

19 . The kit of claim 11 , wherein the dasatinib and the copolymer are present in the amorphous solid dispersion in a w/w ratio of 40:60 to 70:30 (dasatinib: copolymer).

20 . The kit of claim 19 , wherein the copolymer is insoluble in an aqueous medium at pH of 5 or lower, and soluble in an aqueous medium at pH 5.5 or greater.

Assignments (5)
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 14, 2022
From: WERTZ, CHRISTIAN F; CHEN, TZEHAW
To: NANOCOPOEIA, LLC
Reel/Frame 061095/0192 →
Continuity (6)
Continuation 17545370 · Dec 8, 2021
Continuation 17206823 · Mar 19, 2021
Continuation PCTUS2021014742 · Jan 22, 2021
Provisional Application 62965650 · Jan 24, 2020
Provisional Application 63018182 · Apr 30, 2020
Related Publication 20220273657A1 · Sep 1, 2022
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