Claims for Patent: 10,786,511

Summary for Patent: 10,786,511

Title:	Method for treating cancer
Abstract:	The present invention relates to pharmaceutical compositions comprising inhibitor(s) of human histone methyltransferase EZH2, and methods of cancer therapy using the EZH2 inhibitor(s).
Inventor(s):	Keilhack; Heike (Belmont, MA), Truitt; Brett (Cambridge, MA), Suzuki; Yuta (Tokyo, JP), Murase; Tsukasa (Tokyo, JP), Shikata; Futoshi (Tokyo, JP)
Assignee:	Epizyme, Inc. (Cambridge, MA) Eisai R&D Management Co., Ltd. (Tokyo, JP)
Application Number:	15/527,375
Patent Claims:	1. A solid pharmaceutical formulation comprising N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydr- o-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-ca- rboxamide: ##STR00005## in an amount of about 49 wt. %, or a salt of Compound 1 in an amount equivalent to about 49 wt. % of Compound 1, or a combination of Compound 1 and a salt of Compound 1 wherein the combination is present in an amount equivalent to about 49 wt. % of Compound 1; lactose monohydrate in an amount of about 17 wt. %; low-substituted hydroxypropyl cellulose in an amount of about 15 wt. %; sodium starch glycolate in an amount of about 5 wt. %; hydroxypropyl cellulose in an amount of about 4 wt. %; and magnesium stearate in an amount of about 2 wt. %. 2. A solid pharmaceutical formulation consisting of: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydr- o-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-ca- rboxamide: ##STR00006## in an amount of about 40-60 wt. %, or a salt of Compound 1 in an amount equivalent to about 40-60 wt. % of Compound 1, or a combination of Compound 1 and a salt of Compound 1 wherein the combination is present in an amount equivalent to about 40-60 wt. % of Compound 1; lactose monohydrate in an amount of about 10-20 wt. %; low-substituted hydroxypropyl cellulose in an amount of about 11-19 wt. %; sodium starch glycolate in an amount of about 3-7 wt. %; hydroxypropyl cellulose in an amount of about 1-10 wt. %; magnesium stearate in an amount of about 0.5-5 wt. %; and a coating composition in an amount of about 1-10 wt. %. 3. The solid pharmaceutical formulation of claim 2, wherein the coating composition comprises hypromellose, talc, macrogol, titanium dioxide, and iron (III) oxide. 4. The solid pharmaceutical formulation of claim 1, further comprising a coating composition. 5. The solid pharmaceutical formulation of claim 4, wherein the coating composition comprises hypromellose, talc, macrogol, titanium dioxide, and iron (III) oxide. 6. The solid pharmaceutical formulation of claim 1, wherein the pharmaceutical composition comprises Compound 1 in an amount of about 49 wt. %. 7. The solid pharmaceutical formulation of claim 1, wherein the pharmaceutical composition comprises a salt of Compound 1 in an amount equivalent to about 49 wt. % of Compound 1. 8. The solid pharmaceutical formulation of claim 7, wherein the salt of Compound 1 is a hydrobromide salt of Compound 1. 9. The solid pharmaceutical formulation of claim 1, wherein the pharmaceutical composition comprises a combination of Compound 1 and a salt of Compound 1 wherein the combination is present in an amount equivalent to about 49 wt. % of Compound 1. 10. The solid pharmaceutical formulation of claim 9, wherein the salt of Compound 1 is a hydrobromide salt of Compound 1. 11. The solid pharmaceutical formulation of claim 2, consisting of Compound 1 in an amount of about 49 wt. %; lactose monohydrate in an amount of about 10-20 wt. %; low-substituted hydroxypropyl cellulose in an amount of about 11-19 wt. %; sodium starch glycolate in an amount of about 3-7 wt. %; hydroxypropyl cellulose in an amount of about 1-10 wt. %; magnesium stearate in an amount of about 0.5-5 wt. %; and a coating composition in an amount of about 1-10 wt. %. 12. The solid pharmaceutical formulation of claim 2, consisting of a salt of Compound 1 in an amount equivalent to about 49 wt. % of Compound 1; lactose monohydrate in an amount of about 10-20 wt. %; low-substituted hydroxypropyl cellulose in an amount of about 11-19 wt. %; sodium starch glycolate in an amount of about 3-7 wt. %; hydroxypropyl cellulose in an amount of about 1-10 wt. %; magnesium stearate in an amount of about 0.5-5 wt. %; and a coating composition in an amount of about 1-10 wt. %. 13. The solid pharmaceutical formulation of claim 12, wherein the salt of Compound 1 is a hydrobromide salt of Compound 1. 14. The solid pharmaceutical formulation of claim 2, consisting of a combination of Compound 1 and a salt of Compound 1 wherein the combination is present in an amount equivalent to about 49 wt. % of Compound 1; lactose monohydrate in an amount of about 10-20 wt. %; low-substituted hydroxypropyl cellulose in an amount of about 11-19 wt. %; sodium starch glycolate in an amount of about 3-7 wt. %; hydroxypropyl cellulose in an amount of about 1-10 wt. %; magnesium stearate in an amount of about 0.5-5 wt. %; and a coating composition in an amount of about 1-10 wt. %. 15. The solid pharmaceutical formulation of claim 14, wherein the salt of Compound 1 is a hydrobromide salt of Compound 1. 16. The solid pharmaceutical formulation of claim 2, consisting of Compound 1 in an amount of about 49 wt. %; lactose monohydrate in an amount of about 17 wt. %; low-substituted hydroxypropyl cellulose in an amount of about 15 wt. %; sodium starch glycolate in an amount of about 5 wt. %; hydroxypropyl cellulose in an amount of about 4 wt. %; magnesium stearate in an amount of about 2 wt. %; and a coating composition in an amount of about 4 wt. %. 17. The solid pharmaceutical formulation of claim 2, consisting of a salt of Compound 1 in an amount equivalent to about 49 wt. % of Compound 1; lactose monohydrate in an amount of about 17 wt. %; low-substituted hydroxypropyl cellulose in an amount of about 15 wt. %; sodium starch glycolate in an amount of about 5 wt. %; hydroxypropyl cellulose in an amount of about 4 wt. %; magnesium stearate in an amount of about 2 wt. %; and a coating composition in an amount of about 4 wt. %. 18. The solid pharmaceutical formulation of claim 17, wherein the salt of Compound 1 is a hydrobromide salt of Compound 1. 19. The solid pharmaceutical formulation of claim 2, consisting of a combination of Compound 1 and a salt of Compound 1 wherein the combination is present in an amount equivalent to about 49 wt. % of Compound 1; lactose monohydrate in an amount of about 17 wt. %; low-substituted hydroxypropyl cellulose in an amount of about 15 wt. %; sodium starch glycolate in an amount of about 5 wt. %; hydroxypropyl cellulose in an amount of about 4 wt. %; magnesium stearate in an amount of about 2 wt. %; and a coating composition in an amount of about 4 wt. %. 20. The solid pharmaceutical formulation of claim 19, wherein the salt of Compound 1 is a hydrobromide salt of Compound 1.