IP Library Granted Patent US 9,889,116
Granted Patent B2
US 9,889,116 · App. 15/065,344 · Granted Feb 13, 2018

Use of equol for treating androgen mediated diseases

Inventors: Edwin Douglas Lephart (Orem, UT); Trent D. Lund (Wheaton, IL); Robert J. Handa (Fort Collins, CO)
Assignees: BRINGHAM YOUNG UNIVERSITY; COLORADO STATE UNIVERSITY RESEARCH FOUNDATION
A61K31/353A23L33/10A61K8/498A61K9/0014A61K9/0053A61K31/35A61K31/352A61Q7/00A61Q19/08A23V2002/00
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Quick Facts
Patent No.
US 9,889,116
App. No.
15/065,344
Granted
Feb 13, 2018
Kind
B2
Abstract

Equol (7-hydroxy-3(4′hydroxyphenyl)-chroman), the major metabolite of the phytoestrogen daidzein, specifically binds and blocks the hormonal action of 5α-dihydrotestosterone (DHT) in vitro and in vivo. Equol can bind circulating free DHT and sequester it from the androgen receptor, thus altering growth and physiological hormone responses that are regulated by androgens. These data suggest a novel model to explain equol's biological properties. The significance of equol's ability to specifically bind and sequester DHT from the androgen receptor have important ramifications in health and disease and may indicate a broad and important usage for equol in the treatment and prevention of androgen-mediated pathologies. Thus, equol can specifically bind DHT and prevent DHT's biological actions in physiological and pathophysiological processes.

Claims (28)

1. A method of modulating androgen hormone action to ameliorate or enhance at least one condition of the skin or hair of a subject, comprising administering a composition comprising a racemic equol, wherein the racemic equol binds free 5α-dihydrotestosterone and inhibits its binding with the androgen receptor, and wherein ameliorating or enhancing at least one condition of the skin or hair of a subject comprises at least one of:

a) enhancing skin integrity

b) ameliorating or diminishing acne,

c) enhancing anti-photo-aging and skin anti-aging,

d) boosting extracellular matrix proteins,

e) diminishing scalp hair loss, or

f) enhancing the retention of scalp hair in male or female pattern baldness.

2. The method of claim 1 , wherein the composition is an oral composition comprising a dose sufficient to produce a concentration of the racemic equol in the bloodstream of the subject of at least about 0.2 mg equol per kg weight of the subject.

3. The method of claim 1 , wherein the composition is a topical composition comprising from about 0.1% to about 10% racemic equol.

4. The method of claim 1 , wherein the composition is a topical or subdermal composition comprising from about 0.1% to about 10% for diminishing scalp hair loss or enhancing the retention of scalp hair.

5. The method of claim 1 , wherein the composition further comprises a pharmaceutical active or an excipient.

6. The method of claim 1 , wherein the administerin is topically, transdermally, or subdermally.

7. The method of claim 1 , wherein the composition is in a delayed or sustained release formulation.

8. The method of claim 1 , wherein the administering is via a lotion, a spray solution, a foam solution, a pad, a bandage, or a transdermal patch.

9. A method of modulating androgen hormone action to ameliorate or enhance at least one condition of the skin or hair of a subject, comprising administering a composition comprising a racemic equol, wherein the racemic equol binds free 5α-dihydrotestosterone and inhibits its binding with the androgen receptor, and wherein ameliorating or enhancing at least one condition of the skin or hair of a subject comprises at least one of:

a) enhancing skin integrity

b) ameliorating or diminishing acne,

c) enhancing anti-photo-aging and skin anti-aging,

d) boosting extracellular matrix proteins,

e) diminishing scalp hair loss, or

f) enhancing the retention of scalp hair in male or female pattern baldness.

10. The method of claim 9 , wherein the composition is an oral composition comprising a dose sufficient to produce a concentration of the racemic equol in the bloodstream of the subject of at least about 0.2 mg equol per kg weight of the subject.

11. The method of claim 9 , wherein the composition is a topical composition comprising from about 0.1% to about 10% racemic equol.

12. The method of claim 9 , wherein the composition is a topical or subdermal composition comprising from about 0.1% to about 10% for diminishing scalp hair loss or enhancing the retention of scalp hair.

13. The method of claim 9 , wherein the composition further comprises a pharmaceutical active or an excipient.

14. The method of claim 9 , wherein the administering is topically, transdermally, or subdermally.

15. The method of claim 9 , wherein the composition is in a delayed or sustained release formulation.

16. The method of claim 9 , wherein the administering is via a lotion, a spray solution, a foam solution, a pad, a bandage, or a transdermal patch.

Assignments (3)
CONFIRMATORY LICENSE Recorded Jan 3, 2024
From: COLORADO STATE UNIVERSITY RESEARCH FOUNDATION
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 066158/0915 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 2, 2018
From: LEPHART, EDWIN DOUGLAS
To: BRIGHAM YOUNG UNIVERSITY
Reel/Frame 044517/0428 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 2, 2018
From: HANDA, ROBERT J.; LUND, TRENT D.
To: COLORADO STATE UNIVERSITY RESEARCH FOUNDATION
Reel/Frame 044980/0028 →
Continuity (7)
Continuation 14810117 · Jul 27, 2015
Continuation 13903748 · May 28, 2013
Continuation 13442466 · Apr 9, 2012
Continuation 12572791 · Oct 2, 2009
Continuation 10533045
Provisional Application 60422469 · Oct 29, 2002
Related Publication 20160256436A1 · Sep 8, 2016