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US 2022/0031677 A1Published application
Amorphous kinase inhibitor formulations and methods of use thereof
AssigneeDeciphera Pharmaceuticals, LLC
InventorsMichael D. Kaufman, Scott Bone, Corey Bloom, Fred Jordan
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Abstract
Provided herein is an amorphous compound represented by Formula (I): and compositions thereof, which are useful in the treatment of disorders related to the activity of the c-KIT and PDGFRα kinases, and oncogenic forms thereof.
Claims27
A pharmaceutically acceptable composition for orally delivering 50 mg of a compound represented by Formula (I):
- comprising:
- an intragranular blend, wherein the intragranular blend comprises:
- (i) a solid dispersion having 50 mg of the compound wherein the compound is present in amorphous form and hydroxypropyl methyl cellulose acetate succinate;
- (ii) about 25-35% by weight microcrystalline cellulose based on the total amount of the pharmaceutically acceptable composition;
- (iii) about 25-35% by weight of lactose or a hydrate thereof based on the total amount of the pharmaceutically acceptable composition;
- (iv) about 5% by weight of crospovidone based on the total amount of the pharmaceutically acceptable composition;
- (v) about 0.5% by weight of silicon dioxide based on the total amount of the pharmaceutically acceptable composition;
- and
- (vi) about 0.5% by weight of magnesium stearate based on the total amount of the pharmaceutically acceptable composition;
- and
- an extragranular blend, wherein the extragranular blend comprises
- (i) about 0.5% by weight of silicon dioxide based on the total amount of the pharmaceutically acceptable composition;
- and
- (ii) about 0.5% by weight of magnesium stearate based on the total amount of the of the pharmaceutically acceptable composition;
- wherein the pharmaceutically acceptable composition releases at least 80% of the compound after about 10 minutes to after about 40 minutes when the composition is tested in 900 mL sodium acetate buffer at pH 4.5 using a USP Apparatus II (Paddle Method) at 37° C., with a paddle speed of 75 rpm.
12 more elements
A pharmaceutically acceptable composition for orally delivering 50 mg of a compound represented by Formula (I):
- comprising:
- an intragranular blend, wherein the intragranular blend comprises:
- a) a solid dispersion comprising:
- i) 50 mg of the compound, wherein the compound is present in amorphous form, and
- ii) hydroxypropyl methyl cellulose acetate succinate;
- b) microcrystalline cellulose;
- and
- c) lactose or a hydrate thereof,
- and
- an extragranular blend, wherein the extragranular blend comprises a glidant;
- wherein the pharmaceutically acceptable composition releases at least 80% of the compound after about 10 minutes to a after bout 40 minutes when the composition is tested in 900 mL sodium acetate buffer at pH about 4.5 using a USP Apparatus II (Paddle Method) at about 37° C., with a paddle speed of about 75 rpm.
8 more elements
A pharmaceutically acceptable composition for orally delivering 50 mg of a compound represented by Formula (I):
- comprising:
- an intragranular blend, wherein the intragranular blend comprises:
- a) a solid dispersion comprising:
- i) 50 mg of the compound, wherein the compound is present in amorphous form, and
- ii) hydroxypropyl methyl cellulose acetate succinate;
- and
- an extragranular blend, wherein the extragranular blend comprises a glidant;
- wherein the pharmaceutically acceptable composition releases at least 80% of the compound after about 10 minutes to after about 40 minutes when the composition is tested in 900 mL sodium acetate buffer at pH about 4.5 using a USP Apparatus II (Paddle Method) at about 37° C., with a paddle speed of about 75 rpm.
5 more elements
Dependencies are inferred from the claim text.