A New Selective Estrogen Receptor Modulator with Potent Uterine Antagonist Activity, Agonist Activity in Bone, and Minimal Ovarian Stimulation

• Published in: Endocrinology (Philadelphia) Vol. 146; no. 10; pp. 4524 - 4535
• Main Authors: Geiser, Andrew G., Hummel, Conrad W., Draper, Michael W., Henck, Judith W., Cohen, Ilene R., Rudmann, Daniel G., Donnelly, Kevin B, Adrian, Mary D., Shepherd, Timothy A., Wallace, Owen B., McCann, Denis J., Oldham, Samuel W., Bryant, Henry U., Sato, Masahiko, Dodge, Jeffrey A.
• Format: Journal Article
• Language: English
• Published: Bethesda, MD Endocrine Society 01.10.2005; Oxford University Press
• Subjects: 17β-Estradiol; Agonists; Animals; Biological and medical sciences; Bone and Bones - drug effects; Bone and Bones - physiology; Bone loss; Cell Line, Tumor; Estrogen receptors; Estrogens; Ethinyl Estradiol - pharmacology; Ethinylestradiol; Female; Fundamental and applied biological sciences. Psychology; Humans; Hyperplasia; Kinetics; Naphthalenes - pharmacology; Oral administration; Ovarian cancer; Ovariectomy; Ovaries; Ovulation Induction; Piperidines - pharmacology; Rats; Receptors; Receptors, Estrogen - agonists; Receptors, Estrogen - antagonists & inhibitors; Receptors, Estrogen - drug effects; Receptors, Estrogen - physiology; Selective estrogen receptor modulators; Sex hormones; Sexual Maturation; Stimulation; Uterine cancer; Uterus; Uterus - drug effects; Uterus - physiology; Vertebrates: endocrinology; Weight; Osteoarticular system; Ovary; Agonist; Selective estrogen receptor modulator; Uterus; Female genital system; Antagonist; Bone

The use of selective estrogen receptor modulators for the treatment of estrogen-dependent diseases in premenopausal women has been hindered by undesirable ovarian stimulation and associated risks of ovarian cysts. We have identified a selective estrogen receptor modulator compound (LY2066948) that i...