Amorphous kinase inhibitor formulations and methods of use thereof
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.
1. A pharmaceutically acceptable tablet for orally delivering 50 mg of a compound represented by Formula (I):
the tablet comprising:
(i) a solid dispersion having 50 mg of the compound wherein the compound is present in amorphous form and 150 mg hydroxypropyl methyl cellulose acetate succinate;
(ii) 179 mg microcrystalline cellulose;
(iii) 179 mg lactose or a hydrate thereof;
(iv) 30 mg crospovidone;
(v) 6 mg of silicon dioxide; and
(vi) 6 mg of magnesium stearate.
2. A method of treating a gastrointestinal stromal tumor in a patient in need thereof, comprising orally administering to the patient: a pharmaceutically acceptable tablet for orally delivering 50 mg of a compound represented by Formula (I):
the tablet comprising:
(i) a solid dispersion having 50 mg of the compound wherein the compound is present in amorphous form and 150 mg hydroxypropyl methyl cellulose acetate succinate;
(ii) 179 mg microcrystalline cellulose;
(iii) 179 mg lactose or a hydrate thereof;
(iv) 30 mg crospovidone;
(v) 6 mg of silicon dioxide; and
(vi) 6 mg of magnesium stearate.