A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats

…, SA Frank, R Hinklin, SA Jones, G Lewis…

Index: Hummel, Conrad W.; Geiser, Andrew G.; Bryant, Henry U.; Cohen, Ilene R.; Dally, Robert D.; 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. Journal of Medicinal Chemistry, 2005 , vol. 48, # 22 p. 6772 - 6775

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Citation Number: 44

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 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.