Pfizer Inc, Collegeville, PA, Columbia University Medical Center, New York, NY, USA.
Int J Womens Health. 2013 Aug 7;5:465-75. doi: 10.2147/IJWH.S39455. eCollection 2013.
Loss of estrogen production in women during menopause results in a state of estrogen deficiency which has been associated with multiple problems, including vasomotor symptoms, symptoms of vulvovaginal atrophy, bone loss, and difficulties with sleep, mood, memory, and sexual activity. The only treatment option currently available to address multiple postmenopausal symptoms in women with an intact uterus is estrogen/progestin-containing hormone therapy (HT). Concerns surrounding side effects and published data regarding the association of HT with the increased risk for breast cancer have induced a decrease in the number of women seeking, initiating, and continuing this type of therapy. A combination containing bazedoxifene and conjugated estrogens (BZA/CE) maintains the established benefits of estrogen therapy for treatment of postmenopausal vasomotor symptoms, vulvovaginal atrophy, and osteoporosis, while certain estrogenic effects, such as stimulation of the uterus and breast, are antagonized without the side effects associated with HT. BZA/CE has been evaluated in a series of multicenter, randomized, double-blind, placebo-controlled, and active-controlled Phase III trials known as the Selective estrogens, Menopause, And Response to Therapy (SMART) trials. BZA/CE demonstrated clinically meaningful improvements in vasomotor symptoms, vulvovaginal atrophy, and a protective effect on the skeleton. These clinical benefits were associated with an acceptable safety profile and an improved tolerability compared with HT. BZA/CE showed a favorable safety profile on the breast, endometrium, and ovaries. The incidence of venous thromboembolism was low and the risk does not appear to be any greater than for CE alone or BZA alone or greater than HT. The incidence of coronary heart disease and cerebrovascular accidents were similar to placebo. The overall incidence of cancer (including breast cancer) was low and similar to placebo. The SMART trials demonstrate that BZA/CE is an alternative option for treating non-hysterectomized, symptomatic, postmenopausal women.
绝经后女性雌激素产生的丧失会导致雌激素缺乏状态，这种状态与多种问题有关，包括血管舒缩症状、外阴阴道萎缩症状、骨丢失以及睡眠、情绪、记忆和性功能障碍。目前，解决有完整子宫的绝经后妇女多种症状的唯一治疗选择是含有雌激素/孕激素的激素治疗（HT）。对副作用的担忧以及关于 HT 与乳腺癌风险增加的相关数据，导致寻求、开始和继续这种治疗的女性人数减少。含有巴多昔芬和结合雌激素（BZA/CE）的组合保留了雌激素治疗绝经后血管舒缩症状、外阴阴道萎缩和骨质疏松症的既定益处，同时拮抗某些雌激素作用，如子宫和乳房的刺激，而没有与 HT 相关的副作用。BZA/CE 已在一系列多中心、随机、双盲、安慰剂对照和阳性对照 III 期试验中进行了评估，称为选择性雌激素、绝经和治疗反应（SMART）试验。BZA/CE 显示出对血管舒缩症状、外阴阴道萎缩以及对骨骼的保护作用具有临床意义的改善。这些临床益处与可接受的安全性概况和与 HT 相比改善的耐受性相关。BZA/CE 在外阴、子宫和卵巢上显示出有利的安全性概况。静脉血栓栓塞的发生率较低，且风险似乎不比单独使用 CE 或 BZA 或比 HT 更大。冠心病和脑血管意外的发生率与安慰剂相似。癌症（包括乳腺癌）的总发生率较低且与安慰剂相似。SMART 试验表明，BZA/CE 是治疗非子宫切除、有症状的绝经后妇女的替代选择。
