Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Use of antiprogestins for the induction of apoptosis in a programming cell

An anti-progestin and cell death technology, which can be used in medical preparations containing active ingredients, anti-tumor drugs, organic active ingredients, etc., and can solve the problems of unobserved and substantial reduction of S-phase tumor cells

Inactive Publication Date: 2005-07-06
SCHERING AG
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is based on the observation that antiprogestins block tumor cell progression in the G0G1 phase of the cell cycle, resulting in a substantial reduction of tumor cells in S phase
However, this effect was not observed with standard breast cancer tamoxifen therapy, estrogen therapy, or oophorectomy

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Use of antiprogestins for the induction of apoptosis in a programming cell
  • Use of antiprogestins for the induction of apoptosis in a programming cell
  • Use of antiprogestins for the induction of apoptosis in a programming cell

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Dose Response Study in DMBA-Induced Tumor Model

[0053] Materials and methods:

[0054] Immature female Sprague-Dawley rats (49-51 days old; 10 animals / group) were used in this study. Mammary gland tumors were induced by a single oral administration of 10 mg of 7,12-dimethylbenzanthracene (DMBA, Serva / Heidelberg). Will have at least one established tumor (greater than 150mm in size 2 ) rats were treated for 4 weeks by: 1) vehicle control, 2) ovariectomy at the beginning of treatment, 3) antiprogestogen (I), 0,5 mg / kg s.c., 4) antiprogestogen (I ), 2mg / kg s.c., 5) antiprogestogen (I), 5mg / kg s.c., 6) antiprogestogen (I), 10mg / kg s.c., and 7) onasitone, 5mg / kg, s.c., each day processing. The change in tumor area (percentage of initial tumor size) was measured weekly by calipers as a growth inhibition parameter. Statistical analysis of group differences in means was performed using the Kruskal Wallis-test. Further elaboration and evaluation of the DMBA pr...

Embodiment 2

[0059] Example 2: Tumor Growth Inhibition in a Rat NMU-Induced Breast Cancer Model

[0060] Materials and methods:

[0061] Tumors were induced in female Sprague-Dawley rats (obtained from Tierzucht Schönwalde, 50-55 days old) by a single intravenous injection of NMU (nitrosomethylurea, 50 mg / kg). Beginning after 10 days, rats with at least one established tumor were treated for 4 weeks by: 1) vehicle control, 2) ovariectomy at the beginning of treatment, 3) antiprogestin (I), 1.0 mg / kg / day, 4) antiprogestin (I), 0.5mg / kg / day, and 5) onasirdone, 5mg / kg / day. The change in tumor area (percentage of initial tumor size) was measured weekly by calipers as a growth inhibition parameter. Statistical analysis of group differences in means was performed using the Kruskal Wallis-test.

[0062] result:

[0063] In intact control animals, further tumor growth was observed, whereas ovariectomy resulted in complete tumor growth inhibition. Treatment with antiprogestins (I) at doses of...

Embodiment 3

[0066] Example 3: Human T47D breast cancer xenograft in scid mice

[0067] Materials and methods:

[0068] Female Fox Chase scid mice (M & B) were supplemented with estradiol pellets (Innovative Research of America). T47D breast cancer cells obtained from cell culture and suspended in matrigel were implanted into the inguinal region of mice. When the tumor size is about 25mm 2 , start treatment. Treatment is continued until the tumor is suppressed. The experimental groups were: 1) control group (vehicle), 2) ovariectomy, 3) antiprogestin (I), 10 mg / kg s.c. Tumor size was determined with calipers. Kruskal Wallis-test was used for statistical analysis of mean group differences.

[0069] result:

[0070] In the T47D breast cancer model, in contrast to the rapid tumor growth in the control group, ovariectomy caused significant inhibition of tumor growth. image 3 It is clearly shown that s.c. application of 10 mg / kg antiprogestin (I) induces apoptosis in tumor cells. The ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention relates to methods and uses for inducing apoptosis in a cell, in particular a breast cancer cell, by the administration of antiprogestins, in particular the antiprogestin 11 beta -(4-acetylphenyl)-17 beta -hydroxy-17 alpha -(1,1,2,2,2-pentaf luoroeth yl)-estra-4,9-dien-3-one or a pharmaceutically acceptab le derivative or analogue thereof. The invention further relates to a treatment of cancer wherein an indicator of high risk is an increased amount of tumor cells in the S-phase of the cell cycle, said treatment comprising an antiprogestin, in particular the antiprogestin 11 beta -(4-acetylphenyl)-17 beta -hydroxy-17 alpha -(1, 1,2, 2,2- pentafluoroethyl)-estra-4,9-dien-3-one or a pharmaceutically acceptable derivative or analogue thereof.

Description

field of invention [0001] The present invention relates to the use of antiprogestins to induce apoptosis in cells. In particular, the present invention relates to the antiprogestin 11β-(4-acetylphenyl)-17β-hydroxy-17α-(1,1,2,2,2-pentafluoroethyl)-estra-4,9-diene-3 - Use of a ketone or a pharmaceutically acceptable derivative or analogue thereof to induce apoptosis in a cell. The present invention also provides the application of the antiprogestogen in the preparation of a drug for treating a type of cancer, such as breast cancer, whose high-risk indicator is an increase in the number of tumor cells in the S phase of the cell cycle. Background of the invention [0002] Antiprogestogens represent a relatively new class of promising therapeutic agents with marked effects in the treatment of hormone-dependent tumors and other diseases. Although antiprogestins were originally developed for non-surgical termination of pregnancy, some antiprogestins have an additional rather sign...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/57A61P35/00A61P43/00C07J7/00
CPCA61K31/57A61P35/00A61P43/00A61K31/565
Inventor 延斯·霍夫曼罗斯玛丽·利希特纳格哈德·西迈斯特梅尔廷·施奈德乌尔丽克·富尔曼
Owner SCHERING AG
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com