Claims for Patent: 12,097,198

Summary for Patent: 12,097,198

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-pyridazinyl)-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-pyridazinyl)-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-pyridazinyl)-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):	Vijaykumar Reddy RAJASEKHAR, Brendan Mark JOHNSON, David B. MacLean, Lynn Seely, Paul N. MUDD, Jr., Hélène M. Faessel
Assignee:	Sumitomo Pharma Switzerland GmbH , Takeda Pharmaceutical Co Ltd
Application Number:	US17/866,203
Patent Claims:	1. A method of treating prostate cancer in a subject in need thereof, the method comprising: (i) orally administering a loading dose of 360 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject; and (ii) about one day after administering the loading dose, orally administering 120 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject once a day; wherein the subject's serum testosterone concentration is below 50 ng/dL by day 8 of the treatment. 2. The method of claim 1, wherein the subject's serum testosterone concentration is below 50 ng/dL by day 4 of treatment. 3. The method of claim 2, wherein the subject's serum testosterone concentration is below 50 ng/dL within 24 to 48 hours after commencing treatment. 4. The method of claim 1, wherein the subject's serum testosterone concentration is below 20 ng/dL from weeks 5 to 48 of treatment. 5. The method of claim 1, wherein the subject's serum testosterone concentration is below 20 ng/dL within five weeks of commencing treatment. 6. The method of claim 1, wherein the subject's serum testosterone concentration is below 20 ng/dl within three weeks after commencing treatment. 7. The method of claim 1, wherein the subject's serum testosterone concentration is below 20 ng/dL within two weeks after commencing treatment. 8. The method of claim 1, wherein the subject's serum testosterone concentration is below 20 ng/dL within one week after commencing treatment. 9. The method of claim 1, wherein the subject's serum testosterone concentration is below 20 ng/dL within 4 days after commencing treatment. 10. The method of claim 2, wherein the subject's serum testosterone concentration is below 20 ng/dL from weeks 5 to 48 of treatment. 11. The method of claim 2, wherein the subject's serum testosterone concentration is below 20 ng/dL within five weeks of commencing treatment. 12. The method of claim 2, wherein the subject's serum testosterone concentration is below 20 ng/dL within three weeks after commencing treatment. 13. The method of claim 2, wherein the subject's serum testosterone concentration is below 20 ng/dL within two weeks after commencing treatment. 14. The method of claim 2, wherein the subject's serum testosterone concentration is below 20 ng/dL within one week after commencing treatment. 15. The method of claim 1, further comprising: (iii) discontinuing administering N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject, wherein the subject's serum testosterone concentration is at least about 280 ng/dL within about 90 days after discontinuing. 16. The method of claim 15, wherein the subject's serum testosterone concentration is at least about 280 ng/dL within about 8 weeks after discontinuing. 17. The method of claim 15, wherein the subject's serum testosterone concentration is at least about 280 ng/dL within about 4 weeks after discontinuing. 18. The method of claim 2, further comprising: (iii) discontinuing administering N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea to the subject, wherein the subject's serum testosterone concentration is at least about 280 ng/dl within about 90 days after discontinuing. 19. The method of claim 18, wherein the subject's serum testosterone concentration is at least about 280 ng/dL within about 8 weeks after discontinuing. 20. The method of claim 18, wherein the subject's serum testosterone concentration is at least about 280 ng/dL within about 4 weeks after discontinuing.