A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.
Article Details
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Hummel CW, Geiser AG, Bryant HU, Cohen IR, Dally RD, Fong KC, Frank SA, Hinklin R, Jones SA, Lewis G, McCann DJ, Rudmann DG, Shepherd TA, Tian H, Wallace OB, Wang M, Wang Y, Dodge JA
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.
- PubMed ID
- 16250633 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Raloxifene Estrogen receptor alpha Ki (nM) 0.37 7.5 22 Details Raloxifene Estrogen receptor alpha EC 50 (nM) 4.32 7.5 22 Details Raloxifene Estrogen receptor beta Ki (nM) 2.74 7.5 22 Details Raloxifene Estrogen receptor beta EC 50 (nM) 4.32 7.5 22 Details