IP Library › Granted Patent US 11,040,019
Granted Patent B2
US 11,040,019 · App. 16/325,678 · Granted Jun 22, 2021

Selective estrogen-receptor modulators (SERMs) confer protection against photoreceptor degeneration

Inventors: Wenxin Ma (Potomac, MD); Lian Zhao (Kensington, MD); Xu Wang (Falls Church, VA); Wai T. Wong (Philadelphia, PA)
Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
A61K31/138A61B5/398A61B5/4848A61K31/4535A61K31/55A61P27/02
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Quick Facts
Patent No.
US 11,040,019
App. No.
16/325,678
Granted
Jun 22, 2021
Kind
B2
Abstract

Methods are disclosed for treating and/or preventing retinal degeneration is a subject. In some embodiments, the method includes administering to the subject a therapeutically effective amount of a selective estrogen receptor modulator (SERM) to treat the retinal degeneration in the subject. In other embodiments, the SERM is administered orally. In some examples, the SERM is tamoxifen, afimoxifene, raloxifene, bazedoxifene, arzoxifene, desmethylarzoxifene, or a salt or derivative thereof, or combinations thereof.

Claims (18)

1. A method of treating retinal degeneration in a subject, or protecting a subject from retinal degeneration, the method comprising administering to the subject a therapeutically effective amount of a selective estrogen receptor modulator (SERM) to treat the retinal degeneration in the subject, wherein the SERM is one or more of tamoxifen, afimoxifene, raloxifene, bazedoxifene, arzoxifene, desmethylarzoxifene, or a salt thereof, thereby treating the retinal degeneration in the subject, or protecting the subject from retinal degeneration.

2. The method of claim 1 , wherein the SERM is a) tamoxifen or a salt thereof; or b) raloxifene or a salt thereof.

3. The method of claim 1 , wherein the subject has retinitis pigmentosa, acute retinal degeneration, atrophic macular degeneration, or diabetic retinopathy.

4. The method of claim 1 , wherein the SERM is administered orally.

5. The method of claim 3 , wherein the SERM is tamoxifen, or a salt thereof, wherein the subject is human, and wherein the tamoxifen is administered at a dose of about 0.8 mg/kg to about 6.5 mg/kg daily.

6. The method of claim 3 , wherein the SERM is tamoxifen, or a salt thereof, wherein the subject is human, and wherein the tamoxifen is administered orally at a dose of about 3.24 mg/kg to about 6.48 mg/kg daily.

7. The method of claim 3 , wherein the SERM is tamoxifen, or a salt thereof, and wherein the tamoxifen is administered at a dose of 10 mg/kg to 80 mg/kg daily.

8. The method of claim 3 , wherein the SERM is tamoxifen, or a salt thereof, and wherein the tamoxifen is administered orally at a dose of 40 mg/kg to 80 mg/kg daily.

9. The method of claim 1 , wherein the SERM is administered for a minimum of three months.

10. The method of claim 1 , wherein the subject is human.

11. The method of claim 1 , wherein the SERM defers photoreceptor loss, reduces photoreceptor function decrement, reduces visual function loss, and/or suppresses retinal microglial activation and/or suppresses pro-inflammatory cytokine expression.

12. The method of claim 1 , further comprising evaluating the vision of the subject.

13. The method of claim 12 , comprising performing electroretinography on the subject.

14. The method of claim 1 , wherein the subject does not have cancer.

15. The method of claim 1 , wherein the subject does not have breast cancer.

16. The method of claim 1 , wherein the SERM is tamoxifen.

17. The method of claim 1 , further comprising selecting the subject with the retinal degeneration, prior to administering to the subject the therapeutically effective amount of the SERM.

18. The method of claim 1 , wherein the method treats the retinal degeneration in the subject.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 15, 2019
From: WONG, WAI T.; WANG, XU; ZHAO, LIAN; MA, WENXIN
To: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Reel/Frame 048349/0724 →
Continuity (2)
Provisional Application 62377439 · Aug 19, 2016
Related Publication 20190209497A1 · Jul 11, 2019