Use of compositions comprising an estrogenic component for the treatment and prevention of musculoskeletal pain

• US 20060276414A1
• Filed: 05/19/2004
• Published: 12/07/2006
• Est. Priority Date: 05/22/2003
• Status: Abandoned Application

• Current Assignee: Evert Johannes Bunschoten, Herman Jan Tijmen Coelingh Bennink
• Original Assignee: Evert Johannes Bunschoten, Herman Jan Tijmen Coelingh Bennink
• Inventors: Bunschoten, Evert Johannes, Coelingh Bennink, Herman Jan Tijmen
• Application Number:
  US10/557,549
• Publication Number:
  US 20060276414A1
• Time in Patent Office: Days
• US Class Current: 514/26
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 19/00 Drugs for skeletal disorders
• CPC Class Codes: A61P 19/02 for joint disorders, e.g. arthritis, arthrosis

Abstract

The present invention relates to a method of treating or preventing musculoskeletal pain in a mammal receiving administration of an estrogen. suppressant selected from the group consisting of aromatase inhibitors, GnRH analogues, cyclo-oxy-genase 2 (COX-2) inhibitors, 17β-hydroxysteroid dehydrogenase type 1 inhibitors, progestogens, anti-estrogens and combinations thereof, said method comprising the administration of an effective amount of an estrogenic component, wherein the estrogenic component is selected from the group consisting of: substances represented by the following formula (1) in which formula R₁, R₂, R₃, R₄ independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors.

Claims

1-12. -12. (canceled)

13. A method of treating or preventing musculoskeletal pain in a mammal receiving administration of an estrogen suppressant selected from the group consisting of aromatase inhibitors, GnRH analogues, cyclo-oxygenase 2 (COX-2) inhibitors, 17β

-hydroxysteroid dehydrogenase type 1 inhibitors, progestogens, anti-estrogens and combinations thereof, said method comprising administering an estrogenic component in an effective amount to prevent said musculoskeletal pain, said estrogenic component being selected from the group consisting of;

substances represented by the following formula

in which formula R₁, R₂, R₃, R₄ independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms;

precursors capable of liberating a substance according to the aforementioned formula when used in the present method, which precursors are derivatives of the estrogenic substances wherein the hydrogen atom of at least one of the hydroxyl groups has been substituted by an acyl radical of a hydrocarbon carboxylic, sulfonic acid or sulfamic acid of 1-25 carbon atoms;

tetrahydrofuranyl;

tetrahydropyranal;

or a straight or branched chain glycosydic residue containing 1-20 glycosidic units per residue; and

mixtures of one or more of the aforementioned substances and/or precursors.

14. Method according to claim 13, wherein R₃ represents a hydroxyl group or an alkoxy group.

15. Method according to claim 13, wherein at least 3 of the groups R₁, R₂, R₃ and R₄ represent hydrogen atoms.

16. Method according to claim 13, wherein the method comprises the uninterrupted administration of the estrogenic component during a period of at least 5 days.

19. Method according to claim 13, wherein the estrogenic component is administered in an amount of at least 1 μ

g per kg of bodyweight per day.

20. Method according to claim 13, wherein the estrogen suppressant is administered orally, intranasally, transdermally, subcutaneously, intramuscularly, intravenously, intravaginally, intrauterinely, pulmonary, rectally or buccally.

21. Method according to claim 13, wherein the estrogen suppressant is selected from the group consisting of aromatase inhibitors, GnRH analogues, cyclo-oxygenase 2 (COX-2) inhibitors, 17β

-hydroxysteroid dehydrogenase type 1 inhibitors, progestogens and combinations thereof.

22. Method according to claim 21, wherein the estrogen suppressant selected from the group consisting of aromatase inhibitors, GnRH analogues, cyclo-oxygenase 2 (COX-2) inhibitors, 17β

-hydroxysteroid dehydrogenase type 1 inhibitors, progestogens and combinations thereof is administered in an amount effective to reduce the serum concentration of 17β

-estradiol to less than 10 pg/ml.

23. Method according to claim 13, wherein the mammal is suffering from breast cancer, uterine cancer, ovarian cancer, endometriosis, uterine fibroids (leiomyomas), benign prostatic hyperplasia and melanoma.

24. Method according to claim 23, wherein the mammal is suffering from breast cancer.

17. Method according to claim 17, wherein the estrogenic component is administered orally, intranasally, transdermally, subcutaneously, intramuscularly, intravenously, intravaginally, intrauterinely, pulmonary, rectally or buccally.

18. Method according to claim 17, wherein the estrogenic component is administered orally, intravaginally, intrauterinely or transdermally.