Claims for Patent: 10,786,501

Summary for Patent: 10,786,501

Title:	Treatment of prostate cancer
Abstract:	Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyr- idazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-- N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyr- idazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-- N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyr- idazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-- N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.
Inventor(s):	Rajasekhar; Vijaykumar Reddy (Apple Valley, CA), Johnson; Brendan Mark (Chapel Hill, NC), MacLean; David B. (Cambridge, MA), Seely; Lynn (San Mateo, CA), Mudd, Jr.; Paul N. (Cary, NC)
Assignee:	Myovant Sciences GmbH (Basil, CH) Takeda Pharmaceutical Company Limited (Osaka, JP)
Application Number:	16/563,161
Patent Claims:	1. A method for treating prostate cancer in a subject in need thereof, the method comprising: administering to the subject once-daily for at least one day for a first treatment period, an oral load dose formulation having 360 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyr- idazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-- N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; and administering to the subject once-daily for 24 consecutive weeks or greater for a second treatment period, an oral maintenance dose formulation having 120 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyr- idazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-- N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; wherein the subject's follicle stimulating hormone (FSH) is less than or equal to about 2.4 mIU/mL after 24 consecutive weeks of treatment. 2. The method of claim 1, wherein profound castration is achieved. 3. The method of claim 2, wherein the profound castration is achieved within 24 to 48 hours after commencing administration and is maintained until the end of administration. 4. The method of claim 1, wherein time to castration resistance is longer than in a subject receiving GnRH agonist therapy. 5. The method of claim 1, further comprising administering enzalutamide. 6. A method for suppressing one or more sex hormones in a subject having hormone-dependent prostate cancer, the method comprising: administering to the subject once-daily for at least one day for a first treatment period, an oral load dose formulation having 360 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyr- idazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-- N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; and administering to the subject once-daily for 24 consecutive weeks or greater for a second treatment period, an oral maintenance dose formulation having 120 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyr- idazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-- N'-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof; wherein the oral maintenance dose formulation has a PK profile in which mean plasma AUC(0-tau) increases at least 1.5 fold when measured from the first day of the first treatment period to last day of the second treatment period; wherein the sex hormone is FSH; and wherein the subject's FSH is less than or equal to about 2.4 mIU/mL after 24 consecutive weeks of treatment. 7. The method of claim 6, wherein profound castration is achieved. 8. The method of claim 7, wherein the profound castration is achieved within 24 to 48 hours after commencing administration and is maintained until the end of administration. 9. The method of claim 6, wherein time to castration resistance is longer than in a subject receiving GnRH agonist therapy. 10. The method of claim 6, further comprising administering enzalutamide.