Dosing Regimens for Elagolix
OwnerMohamad Shebleyinventor
Life of this patent
Estimating the term…
Abstract
The present invention relates to dosing regimens for GnRH receptor antagonists, and, in particular, dosing regimens for 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-phenylethylamino)-butyric acid (Compound A) or a pharmaceutically acceptable salt thereof, in subjects suffering from, for example, endometriosis, adenomyosis, polycystic ovary syndrome (PCOS), or uterine fibroids, to minimize changes in bone mineral density associated with such GnRH receptor antagonists.
Claims20
A method for treating a female subject with 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, the method comprising:
- administering Compound A or a pharmaceutically acceptable salt thereof to the subject according to a first dosing schedule during a first treatment period;
- and
- administering Compound A or a pharmaceutically acceptable salt thereof to the subject according to a second dosing schedule during a second treatment period, wherein the second dosing schedule comprises a lower dose and/or less frequent administration than the first dosing schedule.
A method for treating a female subject with 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, the method comprising:
- administering Compound A or a pharmaceutically acceptable salt thereof to the subject according to a first dosing schedule during a first treatment period, wherein the first dosing schedule comprises twice daily administration of about 200 mg of Compound A or a pharmaceutically acceptable salt thereof;
- and
- subsequently administering Compound A or a pharmaceutically acceptable salt thereof to the subject according to a second dosing schedule during a second treatment period, wherein the second dosing schedule comprises once daily administration of about 150 mg of Compound A or a pharmaceutically acceptable salt thereof.
A method for reducing the rate of bone mineral density loss in a subject treated with 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, the method comprising
- administering Compound A or a pharmaceutically acceptable salt thereof to the subject according to a first dosing schedule during a first treatment period, wherein the first dosing schedule is associated with a first rate of bone mineral density loss;
- subsequently administering Compound A or a pharmaceutically acceptable salt thereof to the subject according to a second dosing schedule during a second treatment period, wherein the second dosing schedule is associated with a second rate of bone mineral density loss that is reduced relative to the first rate of bone mineral density loss.
A method for treating uterine fibroids in a female subject in need thereof, the method comprising:
- administering 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 to the subject during a treatment period, wherein the treatment period lasts for more than six months;
- and
- co-administering a hormone add-back therapy during the treatment period.
Dependencies are inferred from the claim text.