Women's Health, Pfizer Inc., 500 Arcola Rd., Collegeville, PA 19426, USA.
Pharmaceuticals (Basel). 2012 Sep 4;5(9):899-924. doi: 10.3390/ph5090899.
Menopause is associated with health concerns including vasomotor symptoms, vulvar/vaginal atrophy (VVA), and osteoporosis. Estrogen therapy or combined estrogen-progestin therapy (EPT) are primary treatment options for menopausal symptom relief and osteoporosis prevention. Because EPT has been associated with some safety/tolerability concerns relating to undesirable effects of estrogen and progestin, alternative options are needed. The tissue selective estrogen complex (TSEC) is a novel class of agents pairing a selective estrogen receptor modulator (SERM) with 1 or more estrogens. The TSEC combines the established efficacy of estrogens on menopausal symptoms and bone with the protective effects of a SERM on the reproductive tract. The pairing of bazedoxifene (BZA) with conjugated estrogens (CE) has been evaluated in a series of phase 3 clinical trials. BZA 20 mg/CE 0.45 mg and BZA 20 mg/CE 0.625 mg have shown efficacy in reducing the frequency and severity of hot flushes, relieving VVA symptoms, and maintaining bone mass while protecting the endometrium and breast. These BZA/CE doses have been associated with a favorable safety/tolerability profile, with higher rates of cumulative amenorrhea and lower incidences of breast pain than those reported for EPT. Thus, BZA/CE may be a promising alternative to conventional EPT for treating non-hysterectomized, postmenopausal women.
绝经与健康问题相关,包括血管舒缩症状、外阴/阴道萎缩(VVA)和骨质疏松症。雌激素治疗或雌孕激素联合治疗(EPT)是缓解绝经症状和预防骨质疏松症的主要治疗选择。由于 EPT 与雌激素和孕激素的不良影响相关的一些安全性/耐受性问题有关,因此需要替代选择。组织选择性雌激素复合物(TSEC)是一类新型药物,将选择性雌激素受体调节剂(SERM)与 1 种或多种雌激素结合在一起。TSEC 将雌激素在绝经症状和骨骼方面的既定疗效与 SERM 对生殖道的保护作用结合在一起。将巴多昔芬(BZA)与结合雌激素(CE)配对已在一系列 3 期临床试验中进行了评估。BZA 20mg/CE 0.45mg 和 BZA 20mg/CE 0.625mg 已显示出在减少潮热的频率和严重程度、缓解 VVA 症状以及维持骨量的同时保护子宫内膜和乳房方面的疗效。这些 BZA/CE 剂量与有利的安全性/耐受性特征相关,累积闭经率较高,乳房疼痛发生率低于 EPT 报告的发生率。因此,BZA/CE 可能是治疗非子宫切除、绝经后妇女的传统 EPT 的有前途的替代方案。