Claims for Patent: 10,849,888

Summary for Patent: 10,849,888

Title:	Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer
Abstract:	Described herein are methods of treating non-metastatic castrate-resistant prostate cancer with anti-androgens.
Inventor(s):	Chen; Isan (San Diego, CA)
Assignee:	Aragon Pharmaceuticals, Inc. (San Diego, CA)
Application Number:	16/033,432
Patent Claims:	1. A method of treating non-metastatic castration-resistant prostate cancer in a male human comprising administering an anti-androgen at a dose of about 30 mg per day to about 480 mg per day to a male human in need of such treatment, wherein the anti-androgen is 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2fluoro-N-methylbenzamide, and wherein said method further comprises orchiectomy. 2. The method of claim 1, wherein the non-metastatic castration-resistant prostate cancer is a high risk non-metastatic castration-resistant prostate cancer. 3. The method of claim 1, wherein the 4-[7 (6 cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oc- t-5-yl]-2fluoro-N-methylbenzamide is administered orally to the male human. 4. The method of claim 1, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2fluoro-N-methylbenzamide is administered post orchiectomy. 5. The method of claim 1, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2fluoro-N-methylbenzamide is administered daily to the male human. 6. The method of claim 1, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered orally to the male human at a dose of about 180 mg per day to about 480 mg per day. 7. The method of claim 1, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered orally to the male human at a dose of: (a) about 30 mg per day; (b) about 60 mg per day; (c) about 90 mg per day; (d) about 120 mg per day; or (e) about 240 mg per day. 8. The method of claim 1, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered orally to the male human at a dose of about 240 mg per day. 9. The method of claim 1, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered orally to the male human on a continuous daily dosage schedule. 10. A method of treating non-metastatic castration-resistant prostate cancer in a male human consisting essentially of administering an anti-androgen at a dose of about 30 mg per day to about 480 mg per day to a male human in need of such treatment, wherein the anti-androgen is 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide, and wherein said method further comprises orchiectomy. 11. The method of claim 10, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered orally to the male human at a dose of: (a) about 30 mg per day; (b) about 60 mg per day; (c) about 90 mg per day; (d) about 120 mg per day; or (e) about 240 mg per day. 12. The method of claim 10, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide is administered orally to the male human at a dose of about 240 mg per day. 13. The method of claim 10, wherein the 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspir- o[3.4]oct-5-yl]-2fluoro-N-methylbenzamide is administered post orchiectomy. 14. The method of claim 10, wherein the male human with the high risk non-metastatic castration-resistant prostate cancer has a prostate-specific antigen doubling time (PSADT) that is less than or equal to 10 months. 15. The method of claim 1, wherein administration of the anti-androgen provides an increase in the metastasis-free survival of the male human, relative to the mean survival rate of a population of male humans with the non-metastatic castration-resistant prostate cancer, said population having been treated with a placebo.