Raloxifene, sold under the brand name Evista among others, is a medication used to prevent and treat osteoporosis in postmenopausal women and those on glucocorticoids. See also Raloxifene.
Raloxifene is a selective estrogen receptor modulator (SERM) (see Estrogen receptor) and hence is a mixed agonist and antagonist of the estrogen receptor (ER) in different tissues.[1] It has estrogenic activity in some tissues, such as bone and the liver, and antiestrogenic activity in other tissues, such as the breasts and uterus.[1] Its affinity (Kd) for the ERα is approximately 50 pM, which is similar to that of estradiol.[2] Relative to estradiol (see Estrogens), raloxifene has been reported to possess about 8 to 34% of the affinity for the ERα and 0.5 to 76% of the affinity for the ERβ.[3][4] Raloxifene acts as a partial agonist of the ERα and as a pure antagonist of the ERβ.[5][6] In contrast to the classical ERs, raloxifene is an agonist of the G protein-coupled estrogen receptor (GPER) (EC50 = 10–100 nM), a membrane estrogen receptor.[7][8]
(1err).
. Water molecule shown as red sphere.
Estrogen receptor α complexed with raloxifene and a corepressor peptide
of estrogen receptor α complexed with raloxifene and a corepressor peptide (morph was taken from Gallery of Morphs of the Yale Morph Server).
