title: A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.
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.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
authors.forename: Conrad W
authors.initials: CW
authors.lastname: Hummel
authors.forename: Andrew G
authors.initials: AG
authors.lastname: Geiser
authors.forename: Henry U
authors.initials: HU
authors.lastname: Bryant
authors.forename: Ilene R
authors.initials: IR
authors.lastname: Cohen
authors.forename: Robert D
authors.initials: RD
authors.lastname: Dally
authors.forename: Kin Chiu
authors.initials: KC
authors.lastname: Fong
authors.forename: Scott A
authors.initials: SA
authors.lastname: Frank
authors.forename: Ronald
authors.initials: R
authors.lastname: Hinklin
authors.forename: Scott A
authors.initials: SA
authors.lastname: Jones
authors.forename: George
authors.initials: G
authors.lastname: Lewis
authors.forename: Denis J
authors.initials: DJ
authors.lastname: McCann
authors.forename: Daniel G
authors.initials: DG
authors.lastname: Rudmann
authors.forename: Timothy A
authors.initials: TA
authors.lastname: Shepherd
authors.forename: Hongqi
authors.initials: H
authors.lastname: Tian
authors.forename: Owen B
authors.initials: OB
authors.lastname: Wallace
authors.forename: Minmin
authors.initials: M
authors.lastname: Wang
authors.forename: Yong
authors.initials: Y
authors.lastname: Wang
authors.forename: Jeffrey A
authors.initials: JA
authors.lastname: Dodge
mesh_terms: D000818:Animals; D001665:Binding Sites; D001682:Biological Availability; D002460:Cell Line; D049109:Cell Proliferation; D004958:Estradiol / Q000097:blood; D047628:Estrogen Receptor alpha / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000737:chemistry; D047629:Estrogen Receptor beta / Q000819:agonists / Q000037:antagonists & inhibitors*; D005260:Female; D006801:Humans; D007889:Leiomyoma / Q000188:drug therapy*; D008321:Mammary Glands, Animal / Q000166:cytology / Q000187:drug effects; D008958:Models, Molecular; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009929:Organ Size / Q000187:drug effects; D010053:Ovary / Q000033:anatomy & histology / Q000187:drug effects* / Q000378:metabolism; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D020845:Selective Estrogen Receptor Modulators / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014594:Uterine Neoplasms / Q000188:drug therapy*; D014599:Uterus / Q000033:anatomy & histology / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism
chemical_list: D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; C504960:LY2066948; D009281:Naphthalenes; D010880:Piperidines; D020845:Selective Estrogen Receptor Modulators; D004958:Estradiol