Department of Internal Medicine, Endocrine-Metabolic Sciences and Biochemistry, University of Siena, Siena, Italy.
Clin Interv Aging. 2010 Feb 2;5:19-29. doi: 10.2147/cia.s6083.
Selective estrogen receptor modulators (SERMs) represent a class with a growing number of compounds that act as either estrogen receptor agonists or antagonists in a tissue-specific manner. This article reviews lasofoxifene, a new-generation SERM that has completed phase III development for the prevention and treatment of osteoporosis in postmenopausal women. Consistent with preclinical observations, this new SERM demonstrated improved skeletal efficacy over raloxifene and at an oral dose of 0.5 mg/day was effective in the prevention of both vertebral and nonvertebral fractures in postmenopausal women with osteoporosis. At the same dosage, lasofoxifene treatment also reduced estrogen receptor-positive breast cancer risk and the occurrence of vaginal atrophy, but, like the other SERMs, was associated with hot flushes and an increased risk of venous thromboembolic events. With its increased efficacy on the prevention of nonvertebral fractures than current available SERMs and its positive effects on the vagina, this new compound may represent an alternative and cost-effective therapy for osteoporosis in postmenopausal women.
选择性雌激素受体调节剂（SERMs）是一类化合物，它们以组织特异性方式作为雌激素受体激动剂或拮抗剂发挥作用。本文回顾了 lasofoxifene，这是一种新一代 SERM，已完成用于预防和治疗绝经后妇女骨质疏松症的 III 期开发。与临床前观察一致，这种新型 SERM 在骨骼疗效方面优于 raloxifene，并且在 0.5mg/天的口服剂量下，可有效预防绝经后骨质疏松症妇女的椎体和非椎体骨折。在相同剂量下，lasofoxifene 治疗还降低了雌激素受体阳性乳腺癌的风险和阴道萎缩的发生，但与其他 SERMs 一样，与热潮红和静脉血栓栓塞事件风险增加相关。与目前可用的 SERMs 相比，它在预防非椎体骨折方面的疗效更高，并且对阴道有积极影响，这种新化合物可能是绝经后妇女骨质疏松症的一种替代且具有成本效益的治疗方法。
