Methods of treating heavy menstrual bleeding
AssigneeAbbVie Inc.
InventorsKristof Chwalisz, Laura A. Williams, Rita I. Jain, Janine D. North, Juki Wing-Keung Ng
Life of this patent
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Abstract
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.
Claims16
A method for managing heavy menstrual bleeding in a subject suffering from heavy menstrual bleeding, the method comprising
- orally administering to said subject for a period of at least 84 days
- (a) 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 as a sodium salt, wherein the sodium salt is administered in an amount equivalent to 600 mg per day of the free acid, wherein the sodium salt is administered twice daily in a first dose equivalent to about 300 mg of the free acid and a second dose equivalent to about 300 mg of the free acid;
- (b) 1.0 mg per day of estradiol;
- and
- (c) 0.5 mg per day of norethindrone acetate;
- wherein the method reduces the volume of menstrual blood loss in the subject to less than 80 mL per cycle and by at least 50% from baseline.
A method for managing heavy menstrual bleeding associated with uterine fibroids in a subject in need thereof, the method comprising:
- orally administering to said subject for a period of at least 84 days
- (a) 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 as a sodium salt, wherein the sodium salt is administered in an amount equivalent to 600 mg per day of the free acid,
- wherein the sodium salt is administered twice daily in a first dose equivalent to about 300 mg of the free acid and a second dose equivalent to about 300 mg of the free acid;
- (b) 1.0 mg per day of estradiol, once daily;
- and
- (c) 0.5 mg per day of norethindrone acetate, once daily;
- wherein the method reduces the volume of menstrual blood loss in the subject to less than 80 mL per cycle and by at least 50% from baseline.
A method for managing heavy menstrual bleeding associated with uterine fibroids in a subject in need thereof, the method comprising:
- orally administering to the subject for a period of at least 84 days and not to exceed 24 months
- (1) a first dosage form comprising
- (a) 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 as a sodium salt, wherein the sodium salt is present in the first dosage form in an amount equivalent to 300 mg of the free acid;
- (b) 1.0 mg of estradiol;
- and
- (c) 0.5 mg of norethindrone acetate;
- and
- (2) a second dosage form comprising
- (a) 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 as a sodium salt, wherein the sodium salt is present in the second dosage form in an amount equivalent to 300 mg of the free acid;
- wherein the first and second dosage forms are each administered once daily and the first and second dosage forms are administered in approximately the morning and evening of each day, respectively;
- wherein the method reduces the volume of menstrual blood loss in the subject to less than 80 mL per cycle and by at least 50% from baseline.
A method for managing heavy menstrual bleeding associated with uterine fibroids in a subject in need thereof, the method comprising:
- orally administering to said subject for a period of at least 84 days a three drug regimen comprising:
- (a) 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 as a sodium salt, wherein the sodium salt is administered in an amount equivalent to 600 mg per day of the free acid, wherein the sodium salt is administered twice daily in a first dose equivalent to about 300 mg of the free acid and a second dose equivalent to about 300 mg of the free acid;
- (b) 1.0 mg per day of estradiol, once daily;
- and
- (c) 0.5 mg per day of norethindrone acetate, once daily;
- wherein the method reduces the volume of menstrual blood loss in the subject to less than 80 mL per cycle and by at least 50% from baseline;
- and
- wherein the method limits bone mineral density loss from baseline in the subject to less than 8%.
Dependencies are inferred from the claim text.