METHODS OF TREATING HEAVY MENSTRUAL BLEEDING
The present invention relates to the method of treating heavy menstrual bleeding in a subject with or without uterine fibroids and in need of treatment by administering an effective amount 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 or a pharmaceutically acceptable salt thereof, in combination with estrogens and progestogens.
1 . A method for treating endometriosis-associated pain in a subject in need thereof, the method comprising orally administering to the subject a therapeutically effective amount of 4-((R)-2-[5-(2-fluoro-3 -methoxy-phenyl)-3 -(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2, 6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid or a pharmaceutically acceptable salt thereof.
2 . The method of claim 1 , wherein the therapeutically effective amount is about 150 mg per day.
3 . The method of claim 2 , wherein the 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid or pharmaceutically acceptable salt thereof is administered once per day.
4 . The method of claim 2 , wherein the 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid or pharmaceutically acceptable salt thereof is administered once per day for at least 84 days.
5 . The method of claim 2 , wherein the 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid or pharmaceutically acceptable salt thereof is administered once per day for at least 168 days.
6 . The method of claim 1 , wherein the therapeutically effective amount is about 400 mg per day.
7 . The method of claim 6 , wherein the 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid or pharmaceutically acceptable salt thereof is administered twice per day.
8 . The method of claim 6 , wherein the 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid or pharmaceutically acceptable salt thereof is administered twice per day for at least 84 days.
9 . The method of claim 6 , wherein the 4-((R)-2-[5-(2-fluoro-3-methoxy-phenyl)-3-(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid or pharmaceutically acceptable salt thereof is administered twice per day for at least 168 days.
10 . The method of claim 1 , wherein the pain is pelvic pain.
11 . The method of claim 1 , wherein the pharmaceutically acceptable salt is a sodium salt of 4-((R)-2-[5 -(2-fluoro-3 -methoxy-phenyl)-3-(2-fluoro-6-trifluoromethylbenzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenyl-ethylamino)-butyric acid.
12 . The method of claim 1 , wherein the subject is a subject having moderate to severe endometriosis-associated pain.