[Specific estrogen receptor modulators (SERMs)]

Abstract

PRINCIPLE CHARACTERISTICS: Specific estrogen receptor modulators (SERMs) are non-steroid molecules that maintain some of the agonist properties of estrogens on bone tissue and cardiovascular system, but not their stimulating effects on the gynecological sphere. OLD AND NEW MOLECULES: SERMs were formerly known as "antiestrogens" in reference to their primary inhibition of breast tumor growth. Hence, tamoxifen has been used for many years as adjuvant treatment of breast cancer. However, its long-term use is limited by the risk of endometrial hyperplasia, which has led to the development of new molecules devoid of this side effect. Among these molecules, raloxifen, more specifically reserved for the prevention of osteoporosis in menopausal women, has been the subject of major pre-clinical and clinical developments. THE EFFECTS OF RALOXIFEN: In the prevention of postmenopausal bone loss and vertebral fractures, the effects of raloxifen have been established in several randomized, double-blind studies against placebo, which were the basis of its current marketing authorization. Moreover, raloxifen has a favorable effect on lipid profile and, contrary to oral estrogens, does not increase the C-Reactive protein. Endometrial tolerance is good and it is associated with a significant reduction in the incidence of breast cancer in elderly osteoporotic women. ITS PLACE IN THERAPY: Raloxifen's properties raise the question of its place, together with hormone replacement therapy (HRT), in the management of menopausal women. Its absence of efficacy in the control of the climacteric syndrome does not a priori make it a treatment of choice at the beginning of postmenopausal phase. However, its effects in the prevention of vertebral fracture, its good gynecological tolerance and the fact that it is easy to administer, are arguments for its administration in the prevention of osteoporosis in 60 year-old women or in relay to HRT. Its safety on gynecological level privileges its use in all women exhibiting benign breast or uterine pathologies at the origin of poor tolerance to HRT.