Description
Raloxifene is a selective estrogen receptor modulator (SERM) that exhibits agonist activity in bone and antagonist activity in uterine and breast tissues. Raloxifene is clinically used to prevent osteoporosis in post-menopausal women and to treat ER+ breast cancer. This compound exhibits anti-osteoporotic, anti-parasitic, neuromodulatory, and anticancer chemotherapeutic activities. Raloxifene decreases fracture risk and enhances bone strength in clinical settings. In vitro and in vivo, raloxifene inhibits growth of Leishmania and parasitic burden. Additionally, raloxifene increases uptake of glutamate and expression of GLT-1 in astrocytes. In animal models of breast cancer, this compound decreases expression of EGFR, vascular density, and tumor growth.
References
Karki P, Webb A, Zerguine A, et al. Mechanism of raloxifene-induced upregulation of glutamate transporters in rat primary astrocytes. Glia. 2014 Aug;62(8):1270-83. PMID: 24782323.
Reimão JQ, Miguel DC, Taniwaki NN, et al. Antileishmanial activity of the estrogen receptor modulator raloxifene. PLoS Negl Trop Dis. 2014 May 8;8(5):e2842. PMID: 24810565.
Gallant MA, Brown DM, Hammond M, et al. Bone cell-independent benefits of raloxifene on the skeleton: a novel mechanism for improving bone material properties. Bone. 2014 Apr;61:191-200. PMID: 24468719.
Taurin S, Allen KM, Scandlyn MJ, et al. Raloxifene reduces triple-negative breast cancer tumor growth and decreases EGFR expression. Int J Oncol. 2013 Sep;43(3):785-92. PMID: 23842642.
Gizzo S, Saccardi C, Patrelli TS, et al. Update on raloxifene: mechanism of action, clinical efficacy, adverse effects, and contraindications. Obstet Gynecol Surv. 2013 Jun;68(6):467-81. PMID: 23942473.
