A Selective Estrogen Receptor Modulator Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats
Journal of Medicinal Chemistry2005Vol. 48(22), pp. 6772–6775
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Conrad W. Hummel, Andrew G. Geiser, Henry U. Bryant, Ilene R. Cohen, Robert Dally, Kin Chiu Fong, Scott A. Frank, Ronald J. Hinklin, Scott A. Jones, George C. Lewis, Denis McCann, Daniel G. Rudmann, Timothy A. Shepherd, Hongqi Tian, Owen B. Wallace, Minmin Wang, Yong Wang, Jeffrey A. Dodge
Abstract
The design of a novel selective estrogen receptor modulator (SERM) for the potential treatment of uterine leiomyoma is described. 16 (LY2066948-HCl) binds with high affinity to estrogen receptors alpha and beta (ERalpha and ERbeta, respectively) and is a potent uterine antagonist with minimal effects on the ovaries as determined by serum biomarkers and histologic evaluation.
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