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Last Updated: December 12, 2025

Claims for Patent: 10,420,734


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Summary for Patent: 10,420,734
Title:Method of treating cancer using selective estrogen receptor modulators
Abstract:Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM.
Inventor(s):Suzanne E. Wardell, Erik R. Nelson, Donald P. McDonnell
Assignee: Duke University
Application Number:US15/129,197
Patent Claims: 1. A method of treating an estrogen receptor positive breast cancer in a subject, wherein the estrogen receptor positive breast cancer is resistant to an estrogen receptor modulator, the method comprising administering a composition comprising a compound of (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, wherein the composition is administered daily as a single dose or multi-dose.

2. The method of claim 1, wherein the estrogen receptor positive breast cancer is de novo resistant to the estrogen receptor modulator.

3. The method of claim 1, wherein the resistance to the estrogen receptor modulator is acquired.

4. The method of claim 1, wherein the estrogen receptor modulator is a selective estrogen receptor modulator (SERM).

5. The method of claim 4, wherein the SERM is tamoxifen, idoxifene, raloxifene or ICI 182,780.

6. The method of claim 1, wherein the estrogen receptor modulator is an aromatase inhibitor.

7. The method of claim 6, wherein the aromatase inhibitor is anastrozole, letrozole or exemestane.

8. The method of claim 1, wherein an effective amount of the compound is administered.

9. The method of claim 8, wherein the effective amount is from about 200 mg/day to about 500 mg/day.

10. The method of claim 9, wherein the effective amount is about 400 mg/day.

11. The method of claim 10, wherein the compound is administered by oral administration, intravenous administration, intradermal injection, intramuscular injection or subcutaneous injection.

12. The method of claim 11, wherein the compound is administered by oral administration.

13. The method of claim 12, wherein the estrogen receptor modulator is tamoxifen, idoxifene, raloxifene, ICI 182,780, or an aromatase inhibitor.

14. The method of claim 13, further comprising administering an effective amount of at least one compound selected from the group consisting of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6 inhibitor), an antiestrogen, a ligand of retinoic acid or retinoxic X receptor, an antiprogestin, an antiandrogen, vitamin D or metabolite thereof, a farnesyl transferase inhibitor, a PPARα or gamma agonist and a MAP kinase inhibitor.

15. The method of claim 14, wherein the at least one compound is a CDK4/6 inhibitor.

16. The method of claim 10, wherein the composition is administered daily as a single dose.

17. A method of treating an estrogen receptor positive breast cancer in a subject, wherein the estrogen receptor positive breast cancer is resistant to an estrogen receptor modulator, the method comprising administering an oral composition comprising an effective amount of a compound of (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, wherein the effective amount is from about 200 mg/day to about 500 mg/day.

18. The method of claim 17, wherein the estrogen receptor positive breast cancer is de novo resistant to the estrogen receptor modulator.

19. The method of claim 17, wherein the resistance to the estrogen receptor modulator is acquired.

20. The method of claim 17, wherein the estrogen receptor modulator is a selective estrogen receptor modulator (SERM).

21. The method of claim 20, wherein the SERM is tamoxifen, idoxifene, raloxifene or ICI 182,780.

22. The method of claim 17, wherein the estrogen receptor modulator is an aromatase inhibitor.

23. The method of claim 22, wherein the aromatase inhibitor is anastrozole, letrozole or exemestane.

24. The method of claim 17, wherein the effective amount is about 400 mg/day.

25. The method of claim 24, wherein the estrogen receptor modulator is tamoxifen, idoxifene, raloxifene, ICI 182,780, or an aromatase inhibitor.

26. The method of claim 25, further comprising administering an effective amount of at least one compound selected from the group consisting of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6 inhibitor), an antiestrogen, a ligand of retinoic acid or retinoxic X receptor, an antiprogestin, an antiandrogen, vitamin D or metabolite thereof, a farnesyl transferase inhibitor, a PPARα or gamma agonist and a MAP kinase inhibitor.

27. The method of claim 26, wherein the at least one compound is a CDK4/6 inhibitor.

28. The method of claim 24, wherein the composition is administered daily as a single dose.

29. The method of claim 24, wherein the composition is administered daily as a multi-dose.

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