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Use of epothilones in the treatment of osteoporosis and related diseases

A technology for osteoporosis and epothilone, applied in the field of osteoporosis, can solve problems such as side effects

Inactive Publication Date: 2009-10-07
BAYER SCHERING PHARMA OY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drug treatments lead to significant side effects (e.g. bisphosphonates cause osteonecrosis (Bornstein et al., Schweiz Monatsschr. Zahnmed., 2006; 116(10), 1035-1047)

Method used

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  • Use of epothilones in the treatment of osteoporosis and related diseases
  • Use of epothilones in the treatment of osteoporosis and related diseases
  • Use of epothilones in the treatment of osteoporosis and related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0279] This study aimed to investigate the effect of selected test compounds on the resorption activity of human osteoclasts in vitro. Bone resorption was studied using a model in which bone marrow-derived human osteoclast precursor cells were cultured on bovine bone slices for 7 days and allowed to differentiate into bone resorbing osteoclasts. On day 7, medium was changed, test compounds were added, and mature osteoclasts formed were allowed to resorb bone for an additional 3-day culture period. The activity of tartrate-resistant acid phosphatase 5b was measured in culture medium collected from day 7 as an index of the number of osteoclasts formed during differentiation in each well. After a total of 10 days of culture period, the number of C-terminal cross-linked telopeptides of type I collagen (CTX) was determined from the culture medium as the bone resorption index. Results were expressed as a bone resorption index (CTX at day 10 / TRACP5b at day 7), which describes the me...

Embodiment 2

[0327] test compound

[0328] The test compound used in this example was (1S, 3S, 7S, 10R, 11S, 12S, 16R)-7,11-dihydroxy-3-(2-methyl-benzothiazol-5-yl) -10-(prop-2-en-1-yl)-8,8,12,16-tetramethyl-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-di Ketones (called EPO-477) and paclitaxel.

[0329] A 10 mM stock solution was prepared from test compound EPO-477 by dissolving 10 mg of compound in 1.839 ml of 96% EtOH.

[0330] The test compound paclitaxel was used as a 5 mg / ml (5.855 mM) stock solution. Paclitaxel is commercially available and has been used to treat cancer for over a decade. Appropriately dilute the stock solution to obtain the respective test concentrations required in the assay of osteoclast activity: 2.5nM, 5nM, 7.5nM, 10nM, 15nM, 20nM and 50nM for compound EPO-477 and 2.5nM, 5nM, 10nM, 20nM, 50nM, 100 nM and 200 nM compound paclitaxel.

[0331] research description

[0332] Test compounds were added after osteoclast differentiation was complete on day 7, and matu...

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Abstract

The present invention relates to the use of natural or synthetic Epothilones for the treatment or prophylaxis of diseases caused by a dysbalance of osteoclast and osteoblast activity, especially osteoporosis.

Description

technical field [0001] The present invention relates to the use of natural or synthetic epothilones for the treatment or prevention of diseases associated with a dysbalance of osteoclast and osteoblast activity, especially osteoporosis. Background technique [0002] Osteoporosis and related bone diseases are common diseases in modern society (Sambrook et al., Osteoporosis, Lancet 2006 Jun 17, 367(9527):2001-8). These diseases may be induced by age, other diseases or they may be a side effect of drug therapy with existing drugs (eg statins, aromatase inhibitors). [0003] Several therapeutic approaches have been proposed, including bisphosphonate therapy, hormone therapy, and parathyroid therapy. However, these drug treatments lead to significant side effects (eg bisphosphonates cause osteonecrosis (Bornstein et al., Schweiz Monatsschr. Zahnmed., 2006; 116(10), 1035-1047). [0004] Thus there remains a need for new drugs for the treatment and prevention of osteoporosis and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/427A61P19/10
CPCA61K31/427A61P19/00A61P19/02A61P19/08A61P19/10A61P29/00A61P37/00
Inventor J·霍夫曼S·凯克宁U·克莱尔
Owner BAYER SCHERING PHARMA OY
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