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Compositions and methods for modulating bone mass

A drug and conjugation technology, which can be used in drug combinations, pharmaceutical formulations, bone diseases, etc., and can solve problems such as decreased bone mineral density

Inactive Publication Date: 2007-06-06
BAYLOR COLLEGE OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Current therapies for osteoporosis primarily delay but do not completely reverse loss of bone mineral density

Method used

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  • Compositions and methods for modulating bone mass
  • Compositions and methods for modulating bone mass
  • Compositions and methods for modulating bone mass

Examples

Experimental program
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Effect test

Embodiment Construction

[0026] I. Overview

[0027] The invention features compositions for the bone-targeted delivery of beta-adrenergic antagonists and agonists (collectively referred to herein as "beta-adrenergic agents") and the use of such compositions to modulate bone density and growth Methods. In general, the compositions of the invention provide a beta-adrenergic agent covalently or non-covalently bound to one or more moieties (referred to herein as "bone-targeting moieties"), wherein said The one or more moieties enhance the distribution and / or localization of the beta-adrenergic agent into bone and other osteoblast-containing organs / compartments.

[0028] As described in this application, Applicants identified sympathetic nerve signaling as a key regulator of bone resorption through its ability to regulate the expression of several genes in osteoblasts that favor osteoclast differentiation. This finding, together with previous observations, suggests that the sympathetic nervous system (S...

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Abstract

The instant invention relates to compositions and methods for treating or preventing bone diseases. In certain aspects, the invention provides compositions comprising a beta-adrenergic antagonist or agonist associated to a bone-targeted molecule, as well as methods of modulating bone mass and / or growth in a mammal by administering a composition of the present invention. In other aspects, the invention provides methods of modulating bone mass and / or growth in a mammal by administering a composition comprising a beta2-selective antagonist or agonist.

Description

Background of the invention [0001] Bone remodels frequently throughout the life of an individual, whereby old bone is removed and replaced with new bone. This remodeling process occurs through well-defined cellular processes. Pre-existing bone resorption is mediated by osteoclasts, whereas de novo bone formation is mediated by osteoblasts. Imbalances in remodeling lead to osteoporosis, a disease characterized by low bone mass and microarchitectural deterioration leading to increased fragility. In particular, a relative increase in bone turnover and enhanced osteoclast activity at the expense of loss of osteoblast activity underlies osteoporosis. This condition can be due to a number of factors, including postmenopausal estrogen depletion, drug therapy such as glucocorticoids, transplantation, and other unrelated disorders that affect bone turnover. [0002] Osteoporosis is estimated to affect 200 million women worldwide and often results in immobility and, in some cases, de...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/5377A61K31/138A61P19/10A61K31/165A61P19/08A61P19/00
CPCA61K31/138A61K31/165A61K47/48346B82Y5/00A61K31/5377A61K47/48084A61K47/548A61K47/66A61P19/00A61P19/08A61P19/10A61P43/00
Inventor G·卡森提B·德温斯
Owner BAYLOR COLLEGE OF MEDICINE
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