A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.
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.
Hummel
Conrad W
CW
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA.
Geiser
Andrew G
AG
Bryant
Henry U
HU
Cohen
Ilene R
IR
Dally
Robert D
RD
Fong
Kin Chiu
KC
Frank
Scott A
SA
Hinklin
Ronald
R
Jones
Scott A
SA
Lewis
George
G
McCann
Denis J
DJ
Rudmann
Daniel G
DG
Shepherd
Timothy A
TA
Tian
Hongqi
H
Wallace
Owen B
OB
Wang
Minmin
M
Wang
Yong
Y
Dodge
Jeffrey A
JA
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
D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; C504960:LY2066948; D009281:Naphthalenes; D010880:Piperidines; D020845:Selective Estrogen Receptor Modulators; D004958:Estradiol