Selective oestrogen receptor modulators (SERMs)

Selective oestrogen receptor modulators: an update

“…Until further data become available, it is recommended that raloxifene should be stopped prior to prolonged immobilisation or major elective surgrery. 8 Raloxifene does not improve the vasomotor symptoms of the menopause. Reports of adverse events in clinical trials that compared raloxifene with a placebo showed the overall incidence of hot flushes to be 24.6% in women in the raloxifene group and 18.3% in women in the placebo group.…”

“…6 The incidence of both benign and malignant endometrial pathology was also increased in women treated with tamoxifen. 7 With increased understanding of the function and structure of the oestrogen receptor, 8 the development of compounds with more favourable activity profiles became feasible. The ideal activity profile for a SERM for use in postmenopausal women would have strong oestrogenic effects on the skeleton, the cardiovascular system, the urogenital tract and potentially the central nervous system, while possessing anti-oestrogenic activity in the uterus and the breast.…”

“…This review aims to concentrate on the developments made in our understanding of the action of SERMS since the publication of the review by Kearney and Purdie in the year 2000. 8…”