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
  • 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.