Pharmaceutical Formulations for Treating Endometriosis, Uterine Fibroids, Polycystic Ovary Syndrome or Adenomyosis

A pharmaceutical composition comprising:

• (a) about 20 to about 50% by weight of 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid (Compound A) or a pharmaceutically acceptable salt thereof;
• (b) a binder;
• (c) an anti-gelling agent;
• and
• (d) a water soluble filler.

A solid oral dosage form comprising:

• (a) about 33.2% by weight of sodium 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)butanoate;
• (b) about 16.7% by weight of an alkali metal salt;
• and
• (c) about 51.1% by weight of one or more excipients.

A solid oral dosage form comprising:

• (a) about 33.2% by weight of sodium 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)butanoate;
• (b) about 2.9% by weight of a binder;
• (c) about 16.7% by weight of an alkali metal salt;
• (d) about 41.6% by weight of a water soluble filler;
• (e) about 1.8% by weight of a lubricant;
• and
• (f) about 3.8% by weight of a film-coating.

A method of treating heavy menstrual bleeding and pelvic pain in a woman with symptomatic adenomyosis comprising administering a pharmaceutical composition comprising about 300 mg equivalent of Compound A, wherein said composition includes:

• (a) about 33.2% by weight of sodium 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)butanoate;
• (b) about 16.7% by weight of an alkali metal salt;
• and
• (c) about 51.1% by weight of one or more excipients, wherein the excipients comprise a binder, a water soluble filler, a lubricant, and a film-coating.

A method of treating heavy menstrual bleeding and pelvic pain in a woman with non-dominant adenomyosis comprising administering a pharmaceutical composition comprising about 300 mg equivalent of Compound A, wherein said composition includes:

• a) about 33.2% by weight of sodium 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)butanoate;
• b) about 16.7% by weight of an alkali metal salt;
• and
• c) about 51.1% by weight of one or more excipients, wherein the excipients comprise a binder, a water soluble filler, a lubricant, and a film-coating.