USE OF EQUOL FOR TREATING ANDROGEN MEDIATED DISEASES

• US 20100087519A1
• Filed: 10/02/2009
• Published: 04/08/2010
• Est. Priority Date: 10/29/2002
• Status: Active Grant

• Current Assignee: Children's Hospoital Medical Center, Colorado State University Research Foundation, Brigham Young University (The Church of Jesus Christ of Latter-Day Saints)
• Original Assignee: Children's Hospoital Medical Center, Colorado State University Research Foundation, Brigham Young University (The Church of Jesus Christ of Latter-Day Saints)
• Inventors: Handa, Robert J., Lund, Trent D., Setchell, Kenneth David Reginald, Lephart, Edwin Douglas
• Granted Patent: US 8,153,684 B2
• Time in Patent Office: Days
• US Class Current: 514/456
• CPC Class Codes: A23L 33/10 using additives addition of substantially indigestible substances A23L33/21
• CPC Class Codes: A23V 2002/00 Food compositions, function of food ingredients or processes for food or foodstuffs
• CPC Class Codes: A61K 31/35 having six-membered rings with one oxygen as the only ring hetero atom
• CPC Class Codes: A61K 31/352 condensed with carbocyclic rings, e.g. methantheline cannabinoids A61K31/658
• CPC Class Codes: A61K 31/353 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
• CPC Class Codes: A61K 8/498 having 6-membered rings or their condensed derivatives, e.g. coumarin
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/08 Antiseborrheics
• CPC Class Codes: A61P 17/10 Anti-acne agents
• CPC Class Codes: A61P 17/14 for baldness or alopecia
• CPC Class Codes: A61P 17/16 Emollients or protectives, e.g. against radiation
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: A61P 25/28 : for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 3/00 : Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 : Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 : Antihyperlipidemics
• CPC Class Codes: A61P 3/10 : for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 35/00 : Antineoplastic agents
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/14 : of the thyroid hormones, e.g. T3, T4
• CPC Class Codes: A61P 5/16 : for decreasing, blocking or antagonising the activity of the thyroid hormones
• CPC Class Codes: A61P 5/24 : of the sex hormones
• CPC Class Codes: A61P 5/26 : Androgens
• CPC Class Codes: A61P 5/28 : Antiandrogens
• CPC Class Codes: A61P 5/30 : Oestrogens
• CPC Class Codes: A61P 5/50 : for increasing or potentiating the activity of insulin
• CPC Class Codes: A61P 9/00 : Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/12 : Antihypertensives
• CPC Class Codes: A61Q 19/08 : Anti-ageing preparations
• CPC Class Codes: A61Q 7/00 : Preparations for affecting hair growth

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

1-22. -22. (canceled)

23. A method of modulating androgen hormone action so as to ameliorate at least one condition of the prostate in a subject, comprising

administering equol comprising a non-racemic mixture of R-equol and S-equol enantiomers to the subject.

24. The method of claim 23, wherein the condition of the prostate is benign prostatic hyperplasia or prostate cancer.

25. The method of claim 23, wherein the equol is administered as an oral composition comprising at least 1 mg equol.

26. The method of claim 23, wherein the equol comprises a ratio of S-equol to R-equol from less than 50:

50 to about 1;

99.5.

27. The method of claim 23, wherein the equol comprises a ratio of S-equol to R-equol from greater than about 50:

50 to about 99.5;

1.

28. A method of ameliorating at least one condition of the prostate in a subject, comprising

administering equol comprising a non-racemic mixture of R-equol and S-equol enantiomers.

29. The method of claim 28, wherein the condition of the prostate is benign prostatic hyperplasia or prostate cancer.

30. The method of claim 28, wherein the equol is administered as an oral composition comprising at least 1 mg equol.

31. The method of claim 28, wherein the equol comprises a ratio of S-equol to R-equol from less than 50:

50 to about 1;

99.5.

32. The method of claim 28, wherein the equol comprises a ratio of S-equol to R-equol from greater than about 50:

50 to about 99.5;

1.

33. A method of ameliorating benign prostatic hyperplasia in a subject, comprising administering equol comprising a non-racemic mixture of R-equol and S-equol enantiomers.

34. The method of claim 33, wherein the equol comprises a ratio of S-equol to R-equol from less than 50:

50 to about 1;

99.5.

35. The method of claim 33, wherein the equol comprises a ratio of S-equol to R-equol from greater than about 50:

50 to about 99.5;

1.

36. A method of co-modulating androgen hormone actions and estrogen hormone action so as to ameliorate benign prostatic hyperplasia in a subject, comprising administering equol comprising a non-racemic mixture of R-equol and S-equol enantiomers.

37. The method of claim 36, wherein the equol comprises a ratio of S-equol to R-equol from less than 50:

50 to about 1;

99.5.

38. The method of claim 36, wherein the equol comprises a ratio of S-equol to R-equol from greater than about 50:

50 to about 99.5;

1.

39. A pharmaceutical composition for ameliorating benign prostatic hyperplasia in a subject comprising

equol comprising a non-racemic mixture of R-equol and S-equol enantiomers;

and

at least one of a pharmaceutically acceptable carrier, adjuvant, or excipient.