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

J Med Chem. 2005 Nov 3;48(22):6772-5. doi: 10.1021/jm050723z.

Conrad W Hummel ¹, 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

Affiliations

Affiliation

1 Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.

PMID: 16250633 DOI: 10.1021/jm050723z

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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