A Selective Estrogen Receptor Modulator
Designed for the Treatment of Uterine
Leiomyoma with Unique Tissue
Specificity for Uterus and Ovaries in
Rats

Hummel, Conrad W.; Geiser, Andrew G.; Bryant, Henry U.; Cohen, Ilene R.; D. Dally, Robert; Fong, Kin Chiu; Frank, Scott A.; Hinklin, Ronald; Jones, Scott A.; Lewis, George; McCann, Denis J.; Rudmann, Daniel G.; Shepherd, Timothy A.; Tian, Hongqi; Wallace, Owen B.; Wang, Minmin; Wang, Yong; Dodge, Jeffrey A.

doi:10.1021/jm050723z.s001

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A Selective Estrogen Receptor Modulator Designed for the Treatment of Uterine Leiomyoma with Unique Tissue Specificity for Uterus and Ovaries in Rats

journal contribution

posted on 2005-11-03, 00:00 authored by Conrad W. Hummel, Andrew G. Geiser, Henry U. Bryant, Ilene R. Cohen, Robert D. Dally, Kin Chiu Fong, Scott A. Frank, Ronald Hinklin, Scott A. Jones, George Lewis, Denis J. McCann, Daniel G. Rudmann, Timothy A. Shepherd, Hongqi Tian, Owen B. Wallace, Minmin Wang, Yong Wang, Jeffrey A. Dodge

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 α and β (ERα and ERβ, respectively) and is a potent uterine antagonist with minimal effects on the ovaries as determined by serum biomarkers and histologic evaluation.