Compositions and methods for suppressing endometrial proliferation

A technology of composition and medicine, applied in the field of compositions for inhibiting endometrial hyperplasia, capable of solving problems such as endometrial hyperplasia

Inactive Publication Date: 2015-10-28
APTALIS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is concern that long-term treatment with antiprogestogenic substances may lead to endometrial hyperplasia due to the effects of unopposed estrogens

Method used

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  • Compositions and methods for suppressing endometrial proliferation
  • Compositions and methods for suppressing endometrial proliferation
  • Compositions and methods for suppressing endometrial proliferation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0120] CLAIMS 1. A method of inhibiting endometrial hyperplasia, said method comprising administering to a woman in need thereof an effective amount of a composition comprising a progesterone antagonist.

[0121] 2. The method of embodiment 1, wherein the woman in need thereof is a woman with endometriosis.

[0122] 3. The method of embodiment 1, wherein the composition is administered simultaneously, separately or sequentially with the estrogen or the selective estrogen receptor modulator as part of hormone replacement therapy.

[0123] 4. The method of embodiment 1, wherein the binding affinity of the progesterone antagonist for the progesterone receptor is at least 1.5 times the binding affinity of the progesterone antagonist for the glucocorticoid receptor.

[0124] 5. The method of embodiment 1, wherein progesterone levels in the female do not increase significantly following administration of the composition.

[0125] 6. The method of embodiment 1, wherein estrogen leve...

Embodiment 1

[0180] Example 1. The preparation of the present invention can be made into tablets.

[0181] In order to obtain tablets for use in the practice of the present invention, the following components can be compressed together in a tablet press:

[0182]

[0183] In order to obtain bilayer tablets for use in the practice of the present invention, the following components can be compressed together in a tablet press:

[0184]

[0185] In order to obtain tablets comprising an antiestrogenic substance for use in the practice of the invention, for example, the following components can be compressed together in a tablet press:

[0186]

[0187] To obtain an oily preparation for the practice of the invention, for example, the following ingredients may be mixed together and added to ampoules:

[0188] 100.0mg CDB-4124

[0189] 343.4mg castor oil

[0190] 608.6mg Benzyl Benzoate

Embodiment 2

[0191] Example 2. Compounds of the invention may have only weak anti-glucocorticoid receptor binding activity.

[0192] The ability of some antiprogestogens to bind the rabbit progesterone receptor (rbPR) and glucocorticoid receptor (rbGR) was tested in a receptor binding assay. Briefly, uterus or thymus containing Cytoplasm of PR or GR. For PR binding, mix cytoplasm with 6 nM 1,2-[ 3 H] progesterone (50.0Ci / mmol) was incubated together, and a competitor was added at a concentration of 2-100 nM. For GR binding, mix cytoplasm with 6 nM 6,7-[ 3 H]-dexamethasone (40Ci / mmol) was incubated together, and the competitor was added at a concentration of 2-100 nM. After overnight incubation at 4°C, bound and unbound [ 3 H] Steroids. will contain [ 3 The supernatant of the H]-steroid receptor complex was decanted into vials containing 4 ml of Optifluor (Packard Instrument Co.), vortexed, equilibrated in a liquid scintillation counter for 30 minutes, and then counted for 2 minutes....

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Abstract

The subject matter of the instant invention is pertinent to the field of hormone therapy. More specifically, the subject matter of the instant invention concerns methods of treating estrogen-dependent conditions such as endometrial hyperplasia and endometrial cancer in a female undergoing estrogen and / or selective estrogen receptor modulator (SERM) therapy. The instant invention is also relevant to the suppression of endometrial proliferation. The instant invention is also relevant to the treatment of pain associated with endometriosis. The compositions for practicing the methods, comprising progesterone antagonists are also disclosed. Embodiments of the instant invention also disclose methods for identifying new selective progesterone receptor modulators for practicing disclosed methods of treatment.

Description

[0001] This application is a divisional application of the Chinese patent application 200780039426.6 "composition and method for inhibiting endometrial hyperplasia" filed on October 24, 2007. technical field [0002] The present invention relates to compositions and methods for inhibiting endometrial hyperplasia. More specifically, the present invention relates to compositions comprising one or more progesterone antagonists for use in inhibiting endometrial hyperplasia. [0003] Cross References to Related Applications [0004] This application claims priority to the following patent applications: U.S. Provisional Patent Application No. 60 / 862,632, filed October 24, 2006, and U.S. Provisional Patent Application No. 60 / 885,348, filed January 17, 2007, each Both of said applications are incorporated herein by reference in their entirety. Background technique [0005] Estrogens are a group of hormones necessary for a variety of physiological processes, including uterine and m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/57A61P29/00A61P15/00
Inventor J.S.波多尔斯基
Owner APTALIS PHARMA
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