Alba E, Ragonesi G, Colla F, Mazzoleni A, Farina C
Dipartimenti di Discipline Ginecologiche ed Ostetriche Cattedra B, Università degli Studi, Turin, Italy.
Minerva Ginecol. 2002 Jun;54(3):245-51.
During recent years the development of hormone therapy for the treatment breast neoplasms has seen, in addition to classic aspecific antiestrogens (AE) like tamoxifen (TAM) and to a lesser extent toremifen, a major development of new molecules divided into two groups: the first is the so-called selective estrogen receptor modulators (SERMs), the most important of which is Raloxifen, which mediate estrogen-agonist effects in some tissues and estrogen-antagonist effects in others; the second group includes the aromatase inhibitors (AI), important enzymes for peripheral estrogen conversion. Some studies compare or associate classic AE with the new SERMs and AI, both in adjuvant therapy and in treatment for advanced forms. Other trials assess the anti-osteoporotic activity of some SERMs which present concomitant inhibitory activity on the breast and endometrium.
近年来,除了他莫昔芬(TAM)等经典非特异性抗雌激素药物(AE)以及程度稍轻的托瑞米芬外,用于治疗乳腺肿瘤的激素疗法还出现了两大类新分子的重大进展:第一类是所谓的选择性雌激素受体调节剂(SERM),其中最重要的是雷洛昔芬,它在某些组织中介导雌激素激动作用,而在其他组织中介导雌激素拮抗作用;第二类包括芳香化酶抑制剂(AI),这是外周雌激素转化的重要酶。一些研究在辅助治疗和晚期疾病治疗中,对经典AE与新的SERM和AI进行了比较或关联。其他试验评估了一些SERM的抗骨质疏松活性,这些SERM对乳腺和子宫内膜具有同时抑制活性。