Aprela,一种由巴泽多西芬和共轭马雌激素(Premarin)组成的单片制剂,可用于治疗更年期症状。

Dale W Stovall
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引用次数: 0

摘要

Aprela由辉瑞公司开发,是一种组织选择性雌激素复合物,每日一次,口服,含有选择性雌激素受体调节剂bazedoxifene (BZA)和共轭马雌激素(CE)。Aprela被设计为雌激素和黄体酮联合治疗的替代方案,用于治疗与更年期相关的血管舒缩症状,而不存在与雌激素/黄体酮联合治疗相关的潜在安全性问题,并且耐受性更好。雌激素和BZA都与雌激素受体(ER) α和β结合,但当BZA与ER结合时,结果可能是雌激素的激动或拮抗作用。相反,黄体酮可以对抗子宫内雌激素的作用,但与雌激素一起刺激乳房组织,增加患乳腺癌的风险。在III期临床试验中,Aprela显著降低了血管舒缩症状的数量和严重程度,减少了阴道萎缩,增加了骨矿物质密度。然而,高剂量的BZA倾向于减弱CE的这些积极作用。在本文发表时,没有服用Aprela > 2年的妇女的临床数据,也没有明确的试验来确定Aprela对心血管事件、中风、乳腺癌、静脉血栓栓塞或认知功能风险的影响。然而,在本文发表时,FDA正在考虑批准Aprela用于治疗绝经后妇女血管舒缩症状。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Aprela, a single tablet formulation of bazedoxifene and conjugated equine estrogens (Premarin) for the potential treatment of menopausal symptoms.

Aprela, in development by Pfizer Inc, is a once-daily, orally administered, tissue-selective estrogen complex that contains the selective estrogen receptor modulator bazedoxifene (BZA) and conjugated equine estrogens (CE). Aprela was designed as an alternative to combination estrogen and progestin therapy to treat the vasomotor symptoms associated with menopause without the potential safety concerns associated with combination estrogen/progestin therapy, and with better tolerability. Both estrogens and BZA bind to estrogen receptors (ER)alpha and beta, but when BZA binds to an ER, the result may be an estrogen agonistic or antagonistic effect. In contrast, progestins antagonize the effects of estrogen in the uterus, but along with estrogen, stimulate breast tissue increasing the risk for breast cancer. In phase III clinical trials, Aprela significantly reduced the number and severity of vasomotor symptoms, reduced vaginal atrophy and increased bone mineral density. However, higher doses of BZA tended to attenuate these positive effects of CE. At the time of publication, there were no clinical data from women taking Aprela for > 2 years, and no definitive trials to determine the effects of Aprela on the risks for cardiovascular events, stroke, breast cancer, venous thromboembolism or cognitive function had been completed. Nevertheless, at the time of publication, Aprela was under consideration by the FDA for approval to treat vasomotor symptoms in postmenopausal women.

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