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US 2021/0196692 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.
Claims10
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) about 25-35% by weight microcrystalline cellulose based on the total amount of the pharmaceutical composition;
- and
- c) about 25-35% by weight of lactose or a hydrate thereof based on the total amount of the pharmaceutical composition;
- and
- an extragranular blend, wherein the extragranular blend comprises a glidant.
7 more elements
A pharmaceutically acceptable composition for orally delivering 50 mg of a compound represented by Formula (I):
- comprising:
- a solid dispersion, wherein the solid dispersion comprises:
- i) 50 mg of the compound, wherein the compound is present in amorphous form, and
- ii) hydroxypropyl methyl cellulose acetate succinate;
- wherein the compound and the hydroxypropyl methyl cellulose acetate succinate are present in a ratio of compound:
- hydroxypropyl methyl cellulose acetate succinate from about 30:70 to about 20:80;
- wherein the composition releases at least 80% of the compound after 20 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.
4 more elements
A pharmaceutically acceptable tablet 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 tablet;
- (iii) about 25-35%% by weight of lactose or a hydrate thereof based on the total amount of the tablet;
- (iv) about 5% by weight of crospovidone based on the total amount of the tablet;
- (v) about 0.5% by weight of silicon dioxide based on the total amount of the tablet;
- and
- (vi) about 0.5% by weight of magnesium stearate based on the total amount of the pharmaceutical tablet;
- 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 tablet;
- and
- (ii) about 0.5% by weight of magnesium stearate based on the total amount of the of the tablet.
11 more elements
Dependencies are inferred from the claim text.