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Updated: Jun 26, 2026

Intra-iliac Artery Injection for Efficient and Selective Modeling of Microscopic Bone Metastasis
Published on: September 26, 2016
Bone selective effect of an estradiol conjugate with a novel tetracycline-derived bone-targeting agent
Jason R Neale1, Natali B Richter, Kevyn E Merten
1Department of Pharmacology and Toxicology, University of Louisville, Louisville, KY 40292, USA.
Abstract:
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 (BTE(2)-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 BTE(2)-A1. This novel bone-targeting estradiol delivery system has the potential to improve the safety profile of estradiol in the treatment of osteoporosis.
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