Method of treating estrogen receptor positive carcinoma with 17 α-dihydroequilin

• US 7,005,429 B2
• Filed: 09/26/2001
• Issued: 02/28/2006
• Est. Priority Date: 05/21/1991
• Status: Expired due to Fees

• Current Assignee: Wyeth (Pfizer Inc.)
• Original Assignee: Wyeth (Pfizer Inc.)
• Inventors: Bex, Frederick J., Dey, Michael S., Corbin, Alan
• Primary Examiner(s): Cook, Rebecca
• Application Number:
  US09/962,352
• Publication Number:
  US 20020035101A1
• Time in Patent Office: 1,616 Days
• Field of Search: 514/182
• US Class Current: 514/182
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone

Abstract

This invention provides a method of treating estrogen receptor positive carcinoma in a mammal in need thereof which comprises administering an antineoplastic amount of 17(α-dihydroequilin or a mammalian metabolic conjugate thereof orally, parenterally, transdermally, topically, rectally, intravaginally, intranasally, or intrabronchially. As such, the compounds of this invention are useful in treating estrogen receptor positive carcinomas such as carcinomas of the breast, uterus, ovary, fallopian tube, cervix, vagina, liver, pituitary, central nervous system, hypothalamus, bone, skin, kidney, urethra, prostate, and the like.

Claims

1. A method of treating an estrogen receptor positive carcinoma selected from the group consisting of estrogen receptor positive carcinoma of the breast, uterus, ovary, fallopian tube, cervix, vagina, liver, pituitary, central nervous system, hypothalamus, bone, skin, kidney, urethra, and prostate in a mammal in need thereof which comprises administering to said mammal an effective antineoplastic amount of 17α

-dihydroequilin or a sulfate or glucuronide conjugate thereof orally, parenterally, transdermally, topically, rectally, intravaginally, intranasally, or intrabronchially;

wherein said 17α

-dihydroequilin or a sulfate or glucuronide conjugate thereof is in substantially purified form.

2. The method according to claim 1 in which the administered compound is 17α

-dihydroequilin.

3. The method according to claim 1 in which the administered compound is 17α

-dihydroequilin sulfate.

4. The method according to claim 1 in which the estrogen receptor positive carcinoma is of the breast.

5. The method according to claim 2 in which the estrogen receptor positive carcinoma is of the breast.

6. The method according to claim 3 in which the estrogen positive carcinoma is of the breast.

13. The method according to claim 1 in which said 17 α

-dihydroequilin or sulfate or glucuronide conjugate thereof is combined with one or more pharmaceutically acceptable carriers.

15. The method according to claim 13 in which the administered daily dose of 17α

-dihydroequilin or a sulfate or glucuronide conjugate thereof is from 0.09 μ

g/kg to 100 mg/kg.

16. The method according to claim 15 in which the administered daily dose of 17α

-dihydroequilin or a sulfate or glucuronide conjugate thereof is from 5 mg/kg to 50 mg/kg.

7. A method of preventing the growth of an estrogen receptor positive carcinoma, reducing the size of an estrogen receptor positive carcinoma, or eradicating an estrogen receptor positive carcinoma in a mammal bearing an estrogen receptor positive carcinoma which comprises administering to said mammal an effective antineoplastic amount of 17α

-dihydroequilin or a sulfate or glucuronide conjugate thereof orally, parenterally, transdermally, topically, rectally, intravaginally, intranasally, or intrabronchially;

wherein the estrogen receptor positive carcinoma is selected from the group of an estrogen receptor positive carcinoma of the breast, uterus, ovary, fallopian tube, cervix, vagina, liver, pituitary, central nervous system, hypothalamus, bone, skin, kidney, urethra, and prostate; and

wherein said 17α

-dihydroequilin or a sulfate or glucuronide conjugate thereof is in substantially purified form.

8. The method according to claim 7 in which the administered compound is 17α

-dihydroequilin.

9. The method according to claim 7 in which the administered compound is 17α

-dihydroequilin sulfate.

10. The method according to claim 7 in which the estrogen receptor positive carcinoma is of the breast.

11. The method according to claim 8 in which the estrogen receptor positive carcinoma is of the breast.

12. The method according to claim 9 in which the estrogen receptor positive carcinoma is of the breast.

14. The method according to claim 7 in which said 17 α

-dihydroequilin or sulfate or glucuronide conjugate thereof is combined with one or more pharmaceutically acceptable carriers.

17. The method according to claim 14 in which the administered daily dose of 17α

-dihydroequilin or a sulfate or glucuronide conjugate thereof is from 0.09 μ

g/kg to 100 mg/kg.

18. The method according to claim 17 in which the administered daily dose of 17α

-dihydroequilin or a sulfate or glucuronide conjugate thereof is from 5 mg/kg to 50 mg/kg.