US 12,168,014 B2
Method for treating cancer
Heike Keilhack, Belmont, MA (US); Brett Truitt, Cambridge, MA (US); Yuta Suzuki, Tokyo (JP); Tsukasa Murase, Tokyo (JP); and Futoshi Shikata, Tokyo (JP)
Assigned to Epizyme, Inc., Cambridge, MA (US); and Eisai R&D Management Co., Ltd., Tokyo (JP)
Filed by Epizyme, Inc., Cambridge, MA (US); and Eisai R&D Management Co., Ltd., Tokyo (JP)
Filed on Aug. 20, 2020, as Appl. No. 16/998,144.
Application 16/998,144 is a division of application No. 15/527,375, granted, now 10,786,511, previously published as PCT/US2015/061194, filed on Nov. 17, 2015.
Claims priority of provisional application 62/251,903, filed on Nov. 6, 2015.
Claims priority of provisional application 62/166,572, filed on May 26, 2015.
Claims priority of provisional application 62/080,985, filed on Nov. 17, 2014.
Prior Publication US 2021/0060030 A1, Mar. 4, 2021
Int. Cl. A61K 9/20 (2006.01); A61K 9/00 (2006.01); A61K 9/28 (2006.01); A61K 31/5377 (2006.01); A61P 35/00 (2006.01)
CPC A61K 31/5377 (2013.01) [A61K 9/0053 (2013.01); A61K 9/2013 (2013.01); A61K 9/2018 (2013.01); A61K 9/2027 (2013.01); A61K 9/2054 (2013.01); A61K 9/2059 (2013.01); A61K 9/2077 (2013.01); A61K 9/2095 (2013.01); A61K 9/2846 (2013.01); A61K 9/2893 (2013.01); A61P 35/00 (2018.01); A61K 9/2004 (2013.01)] 62 Claims
OG exemplary drawing
 
1. A method of treating a solid tumor or B cell lymphoma, comprising administering to a human subject in need thereof a solid pharmaceutical formulation comprising, in each case relative to the total weight of the solid pharmaceutical formulation, N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3 -yl) methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)-[1,1′-biphenyl]-3-carboxamide:

OG Complex Work Unit Chemistry
in an amount of about 40-60 wt. %, or a pharmaceutically acceptable salt of Compound 1 in an amount equivalent to about 40-60 wt. % of Compound 1, or a combination of Compound 1 and a pharmaceutically acceptable salt of Compound 1 wherein the combination is present in an amount equivalent to about 40-60 wt. % of Compound 1;
a diluent comprising lactose monohydrate;
a disintegrant in an amount of about 15-25 wt. % comprising low-substituted hydroxypropyl cellulose, sodium starch glycolate, or a combination thereof;
a binder in an amount of about 1-10 wt. % comprising hydroxypropyl cellulose; and
a lubricant in an amount of about 0.5-5 wt. % comprising magnesium stearate; wherein the solid pharmaceutical formulation provides a maximum plasma concentration of Compound 1 at a median Tmax of from about 1 hour to about 2 hours after multiple dosing for 15 days.