[Selective estrogen receptor modulators (SERMs)].
Toshio Matsumoto
Abstract
Toshio Matsumoto
Abstract
Selective estrogen receptor modulators (SERMs) bind to estrogen receptor (ER) and develop tissue-selective actions as estrogen agonists or antagonists. As such, SERMs have been developed to exert estrogen-like beneficial effects against some disorders including osteoporosis, while reducing estrogen-related risks, including breast cancer. Prevention of vertebral fractures by a SERM, raloxifene (RLX), in osteoporotic postmenopausal women has been well established. RLX does not increase or decrease cardiovascular events, overall mortality, cardiovascular mortality or the overall number of strokes, but there appears to be a small increase in stroke mortality. Both RLX and tamoxifen similarly reduce the risk of ER-positive invasive breast cancer. At the same time, RLX treatment is associated with 36% fewer uterine cancer incidence and 29% less thromboembolic events. Keeping these results in mind, it is our responsibility to critically evaluate and decide timing and length of treatment, as well as subjects with benefits or risks for the treatment of osteoporosis by SERMs.
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Selective estrogen receptor modulators (SERMs) bind to estrogen receptor (ER) and develop tissue-selective actions as estrogen agonists or antagonists. As such, SERMs have been developed to exert estrogen-like beneficial effects against some disorders including osteoporosis, while reducing estrogen-related risks, including breast cancer. Prevention of vertebral fractures by a SERM, raloxifene (RLX), in osteoporotic postmenopausal women has been well established. RLX does not increase or decrease cardiovascular events, overall mortality, cardiovascular mortality or the overall number of strokes, but there appears to be a small increase in stroke mortality. Both RLX and tamoxifen similarly reduce the risk of ER-positive invasive breast cancer. At the same time, RLX treatment is associated with 36% fewer uterine cancer incidence and 29% less thromboembolic events. Keeping these results in mind, it is our responsibility to critically evaluate and decide timing and length of treatment, as well as subjects with benefits or risks for the treatment of osteoporosis by SERMs.
Key concepts: Raloxifene, Selective estrogen receptor modulator, Tamoxifen, Medicine, Osteoporosis, Estrogen, Estrogen receptor, Breast cancer