Trémollières Florence, Lopes Patrice
Unité de ménopause et maladies osseuses métaboliques, service d'endocrinologie, CHU Rangueil, Toulouse (31).
Presse Med. 2002 Sep 7;31(28):1323-8.
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.
特定雌激素受体调节剂（SERM）是非甾体分子，在骨组织和心血管系统上保持一些雌激素的激动剂特性，但对妇科领域没有刺激作用。
SERM以前被称为“抗雌激素”，是因其对乳腺肿瘤生长的主要抑制作用。因此，他莫昔芬多年来一直用作乳腺癌的辅助治疗药物。然而，其长期使用受到子宫内膜增生风险的限制，这促使了无此副作用的新分子的研发。在这些分子中，雷洛昔芬更专门用于预防绝经后妇女的骨质疏松症，是主要临床前和临床研究的对象。
在预防绝经后骨质流失和椎体骨折方面，雷洛昔芬的作用已在多项针对安慰剂的随机、双盲研究中得到证实，这些研究是其当前上市许可的基础。此外，雷洛昔芬对血脂状况有有利影响，与口服雌激素相反，它不会增加C反应蛋白。子宫内膜耐受性良好，且与老年骨质疏松妇女乳腺癌发病率的显著降低有关。
雷洛昔芬的特性引发了它与激素替代疗法（HRT）在绝经后妇女管理中的地位问题。它在控制更年期综合征方面缺乏疗效，这使其在绝经后初期并非首选治疗方法。然而，它在预防椎体骨折方面的作用、良好的妇科耐受性以及易于给药的特点，使其成为60岁妇女预防骨质疏松或作为HRT接力治疗的依据。其在妇科层面的安全性使其更适合用于所有因对HRT耐受性差而患有良性乳腺或子宫疾病的女性。
