Claims for Patent: 10,426,782

Summary for Patent: 10,426,782

Title:	Pharmaceutical formulations of a pan-RAF kinase inhibitor and processes for their preparation
Abstract:	The invention relates to a pharmaceutical composition comprising Compound 1 or a pharmaceutically acceptable salt thereof for the treatment of cancer and a process for its preparation. The invention also relates to administering the pharmaceutical composition to a patient according to an intermittent dosing regimen.
Inventor(s):	Brake Rachael L., Bozon Viviana, Chow Ching-Kuo J., Dinunzio James C., Galvin Katherine M., Kannan Karuppiah, Kodono Yuki, Xu Qunli
Assignee:	MILLENNIUM PHARMACEUTICALS, INC.
Application Number:	US15128714
Patent Claims:	1. A pharmaceutical composition comprising:(1) 10% to 50% w/w of a solid dispersion extrudate comprising:(a) about 40% w/w of (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide, or a pharmaceutically acceptable salt thereof, and(b) about 60% w/w of copovidone; and(2) 90% to 50% w/w of one or more pharmaceutically acceptable excipients,wherein the solid dispersion extrudate comprises <3% w/w of (S)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide.2. The pharmaceutical composition of claim 1 , which comprises croscarmellose sodium.3. The pharmaceutical composition of claim 1 , which comprises colloidal silicon dioxide.4. The pharmaceutical composition of claim 1 , which comprises magnesium stearate.5. The pharmaceutical composition of claim 1 , which comprises microcrystalline cellulose.6. A process for preparing a pharmaceutical composition of claim 1 , which comprises:(i) extruding a mixture of (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide, or a pharmaceutically acceptable salt thereof, and copovidone to form a solid dispersion extrudate; and(ii) blending the resulting solid dispersion extrudate with one or more pharmaceutically acceptable excipients,wherein the solid dispersion extrudate comprises <3% w/w of (S)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide.