IP Library › Granted Patent US 12,263,142
Granted Patent B2
US 12,263,142 · App. 18/457,567 · Granted Apr 1, 2025

Method of treating cancer using selective estrogen receptor modulators

Inventors: Suzanne E. Wardell (Durham, NC); Erik R. Nelson (Champaign, IL); Donald P. McDonnell (Chapel Hill, NC)
Assignee: Duke University
A61K31/137A61K9/0019A61K31/136A61K31/138A61K31/40A61K31/4196A61K31/4535A61K31/565A61K31/5685A61K45/06C07C217/78C07C217/84A61K2121/00
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Quick Facts
Patent No.
US 12,263,142
App. No.
18/457,567
Granted
Apr 1, 2025
Kind
B2
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.

Claims (14)

1. A method of treating estrogen receptor positive breast cancer brain metastasis in a subject, the method comprising administering a compound of (R)-6-{2-{ethyl [4-(2-ethylaminoethyl) benzyl] amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, wherein the estrogen receptor positive breast cancer brain metastasis is resistant to an aromatase inhibitor.

2. The method of claim 1 , wherein the compound is administered at a dose of about 10 mg/day to about 500 mg/day.

3. The method of claim 2 , wherein the composition is administered as a single dose or a multi-dose.

4. The method of claim 3 , wherein the composition is administered as a single dose.

5. The method of claim 1 , wherein the compound is administered by oral administration, intravenous administration, intradermal injection, intramuscular injection or subcutaneous injection.

6. The method of claim 1 , 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 PPARa or gamma agonist and a MAP kinase inhibitor.

7. The method of claim 1 , wherein the aromatase inhibitor is anastrozole, letrozole or exemestane.

8. A method of treating estrogen receptor positive breast cancer brain metastasis in a subject, the method comprising administering a composition comprising (R)-6-{2-{ethyl [4-(2-ethylaminoethyl) benzyl] amino}-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol, wherein the estrogen receptor positive breast cancer brain metastasis is resistant to an aromatase inhibitor.

9. The method of claim 8 , wherein the composition comprises the compound at a dose of about 10 mg to about 500 mg.

10. The method of claim 9 , wherein the composition is administered as a single dose or a multi-dose.

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

12. The method of claim 8 , wherein the composition is administered by oral administration, intravenous administration, intradermal injection, intramuscular injection or subcutaneous injection.

13. The method of claim 8 , 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 PPARa or gamma agonist and a MAP kinase inhibitor.

14. The method of claim 8 , wherein the aromatase inhibitor is anastrozole, letrozole or exemestane.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 6, 2025
From: WARDELL, SUZANNE E.; NELSON, ERIK R.; MCDONNELL, DONALD P.
To: DUKE UNIVERSITY
Reel/Frame 069749/0881 →
Continuity (7)
Continuation 17558731 · Dec 22, 2021
Continuation 16549828 · Aug 23, 2019
Continuation 15129197
Continuation In Part 14512061 · Oct 10, 2014
Provisional Application 62129379 · Mar 6, 2015
Provisional Application 61971627 · Mar 28, 2014
Related Publication 20230398085A1 · Dec 14, 2023
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