Bone selective effect of an estradiol conjugate with a novel tetracycline-derived bone-targeting agent
摘要:
In this study a novel bone-targeting agent containing elements of the tricarbonylmethane system of ring A of tetracycline was developed and was shown to bind to the mineral constituent of bone, hydroxyapatite. Conjugation of this bone-targeting agent to estradiol resulted in a bone-targeted estrogen (BTE2-A1) with an enhanced ability to bind to hydroxyapatite. In an ovariectomized rat model of osteoporosis a partial separation of the skeletal effects of estradiol from the uterine effects was observed following subcutaneous administration of BTE2-A1. This novel bone-targeting estradiol delivery system has the potential to improve the safety pro. le of estradiol in the treatment of osteoporosis. (c) 2008 Elsevier Ltd. All rights reserved.
Compounds for diagnosis, treatment and prevention of bone injury and metabolic disorders
申请人:Pierce M. William
公开号:US20050143366A1
公开(公告)日:2005-06-30
The present invention relates to compounds of the formula
or pharmaceutically acceptable salts thereof useful for the prophylaxis and treatment of degenerative bone disorders and for the acceleration of bone healing.