Claims for Patent: 12,692,251

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Summary for Patent: 12,692,251

Title:	Pralsetinib pharmaceutical compositions
Abstract:	The present disclosure relates to pharmaceutical composition comprising 1) an amorphous solid dispersion comprising pralsetinib, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable hydrophilic polymer; and 2) an effervescent couple; and crystalline forms of pralsetinib and pralsetinib hydrochloride salt, which are useful as a RET selective inhibitors. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline forms and methods of using said compositions in the treatment of various disorders.
Inventor(s):	Joshua Waetzig, Gordon D. Wilkie, Debra L. Mazaik, Csanad M. Varga, Lia Rogal, Lauren MacEachern, Kimberly Jean Miller, Shellie Rigby-Singleton, Ian A. Barker, Robert J. Harris, Aimee J. Spenceley, Dipak Gordhan
Assignee:	Catalent Nottingham Ltd , Rigel Pharmaceuticals Inc
Application Number:	US18/000,166
Patent Claims:	1. An immediate release oral dosage form comprising: a) an amorphous solid dispersion comprising: pralsetinib, or a pharmaceutically acceptable salt thereof, and hydroxypropyl methylcellulose E3, wherein the pralsetinib or an equivalent amount of pharmaceutically acceptable salt thereof and the hydroxypropyl methyl cellulose E3 are in about a 1:1 weight ratio; b) an effervescent couple comprising about 3 to about 13 w/w % citric acid and about 7 to about 30 w/w % sodium bicarbonate; wherein w/w % is based on the total weight of the oral dosage form; c) a diluent; and d) moisture scavenger and a lubricant, wherein the immediate release oral dosage form comprises the amorphous solid dispersion from about 25% to about 65% percent by weight of the immediate release oral dosage form, based on the total weight of the oral dosage form, and the immediate release oral dosage form is a tablet or a capsule. 2. The oral dosage form of claim 1, wherein the amorphous solid dispersion comprises about 30 mg, about 50 mg, about 60 mg or about 100 mg of pralsetinib or an equivalent amount of a pharmaceutically acceptable salt thereof. 3. The composition of claim 1, wherein the dosage form is a capsule, wherein the capsule disintegrates in about 7 to 15 minutes using USP <701>, with Basket Type A and a disc with a maintained temperature at 37° C.±2° C. 4. The composition of claim 1, wherein the dosage form is a capsule, wherein at least 80% of the pralsetinib is released in about 120 minutes using USP <711> with a Type 2 Apparatus with a media containing 900 mL pH 6.8 sodium phosphate buffer with 0.5% CTAB and a paddle speed of 75 rpm±2 rpm. 5. An immediate release oral dosage form comprising: a) about 55 w/w % of an amorphous solid dispersion comprising: pralsetinib, or a pharmaceutically acceptable salt thereof, and hydroxypropyl methylcellulose E3, wherein the pralsetinib or an equivalent amount of pharmaceutically acceptable salt thereof and the hydroxypropyl methyl cellulose E3 are in about a 1:1 weight ratio; b) an effervescent couple comprising about 9 w/w % citric acid and about 22 w/w % sodium bicarbonate; c) about 9 w/w % microcrystalline cellulose; d) about 4 w/w % pregelatinized starch; and e) about 1 w/w % magnesium stearate, wherein w/w % is based on the total weight of the oral dosage form, and the immediate release oral dosage form is a tablet or a capsule.