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A method of treating breast cancer with androgen receptor antagonists

An androgen receptor, antagonist technology, applied in the field of prevention and treatment of individuals, can solve the problems of ineffectiveness, danger and high cost

Inactive Publication Date: 2006-04-26
GTX INCORPORATED
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Currently available therapies for breast cancer are toxic, dangerous, costly, and many are ineffective, especially in the treatment of metastatic disease

Method used

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  • A method of treating breast cancer with androgen receptor antagonists
  • A method of treating breast cancer with androgen receptor antagonists
  • A method of treating breast cancer with androgen receptor antagonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0250] Extended cytotoxicity studies of compounds in different cell lines

[0251] Different prostate cancer cell lines (DU145, PC-3, TSU, PPC-1 and LNCaP), breast cancer cell line (MCF-7), other cancer cell lines (MCF- 7) and the control cell line (CV-1), the IC of I-31, I-29, S-NTBA and Compound V 50 As shown in Table 2A and B.

[0252] Table 2A - Prostate cancer cell lines

[0253]

[0254] Table 2B - Other cancer cell lines and controls

[0255]

Embodiment 2

[0257] Effects of Compounds on Apoptosis in Different Cell Lines

[0258] Determination of I-31, I-29, S-NTBA and compound V in different prostate cancer cell lines (DU145, PC-3, TSU, PPC-1 and LNCaP), breast cancer cell line (MCF-7) and other cancer cell lines (TCCSUP, HT-29) and the ability to induce apoptosis in the control cell line (CV-1), the results are shown in Table 3.

[0259] table 3

[0260] Apoptosis by Histone assay

[0261]

Embodiment 3

[0263] Sensitivity of Androgen Receptor Responsive Cells to Compound V

[0264] The relative androgen receptor (AR) expression of various cell lines is shown in Table 4. Both the LNCaP prostate and MCF-7 breast cancer cell lines express androgen receptors, whereas the prostate cancer cell lines PC-3 and Du145 and the African green monkey kidney epithelial CV-1 cells do not express androgen receptors (Chlenski, MacIndoe, Warriar , Webber 1 & 2).

[0265] cell line

LNCaP

PC-3

Du 145

MCF-7

CV-1

AR

+

-

-

+

-

Mutation

+

N / A

N / A

-

N / A

mutation

T877A

N / A

N / A

N / A

N / A

Methylation of the AR promoter

-

powerful

completely

-

N / A

transcription

normal

-

-

normal

-

PSA expression

+

-

-

+

-

Other steroid receptors:

EGF / TGF-α

FGF...

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PUM

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Abstract

The present invention relates to the prevention and treatment of breast cancer in an individual, such as a female individual. Accordingly, the present invention provides the following methods: by administering to a subject a therapeutically effective amount of an androgen receptor antagonist and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, drug product, hydrate, N - oxides, crystals, polymorphs, prodrugs or any combination thereof, a) to treat a subject with breast cancer; b) to prevent, suppress, suppress or reduce the incidence of breast cancer in a subject; c) to delay the progression of breast cancer development of breast cancer in an individual; d) preventing recurrence of breast cancer in an individual; e) treating recurrence of breast cancer in an individual with breast cancer; and / or f) treating, preventing, suppressing or inhibiting metastasis in an individual with breast cancer, as described herein.

Description

technical field [0001] The present invention relates to the prevention and treatment of breast cancer in an individual, such as a female individual. More specifically, the present invention provides the following methods: by administering to a subject a therapeutically effective amount of an androgen receptor antagonist and / or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, drug product, hydration substances, N-oxides, crystals, polymorphs, prodrugs, or any combination thereof, a) treating an individual with breast cancer; b) preventing, suppressing, inhibiting or reducing the incidence of breast cancer in an individual; c) delaying the development of breast cancer There is breast cancer development in the individual of breast cancer; d) prevent breast cancer recurrence in individual; E) treat breast cancer recurrence in individual with breast cancer; And / or f) treat, prevent, suppress or suppress the metastasis of individual with breast cancer, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/21A61KA61K31/165A61K31/26A61K31/277A61K31/32A61K31/66A61P35/00
CPCA61K31/21A61K31/26A61K31/66A61P35/00A61P43/00
Inventor 米切尔·S.·斯坦纳詹姆斯·T.·多尔顿杜安·D.·米勒卡伦·A.·韦韦尔卡
Owner GTX INCORPORATED
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