Adis, a Wolters Kluwer Business, Auckland, New Zealand.
Drugs. 2011 Nov 12;71(16):2193-212. doi: 10.2165/11207420-000000000-00000.
Bazedoxifene (Conbriza®, Viviant®) is the first third-generation selective estrogen receptor modulator (SERM) and it is approved for the treatment of postmenopausal osteoporosis in the EU and Japan. Bazedoxifene contains an indole-based core binding domain that binds with high affinity to estrogen receptors and exhibits favourable effects on bone and lipid profiles, with no clinically relevant endometrial or breast stimulation. Oral bazedoxifene once daily reduced the incidence of new vertebral fractures in patients with postmenopausal osteoporosis in a large, well designed trial of 3 years' duration; both bazedoxifene and raloxifene were significantly more effective than placebo. Neither bazedoxifene nor raloxifene reduced the incidence of nonvertebral fractures in the overall study population; however, bazedoxifene, but not raloxifene, reduced the rate of nonvertebral fractures in high-risk patients. Moreover, data from patients who continued to receive the drug during a 2-year extension phase of this trial indicate that bazedoxifene continues to provide protection against new vertebral fractures for up to 5 years. Bazedoxifene also increases bone mineral density and reduces the levels of bone turnover markers. Bazedoxifene was generally well tolerated and did not detrimentally affect the reproductive tract or breast tissue in clinical trials, thereby demonstrating a favourable risk-benefit profile. A pharmacoeconomic analysis conducted from an EU perspective predicted bazedoxifene to be cost effective in some EU countries. Therefore, bazedoxifene presents another useful option for the treatment of postmenopausal osteoporosis, especially in those at high risk for osteoporotic fracture.
巴多昔芬(康布瑞扎®,唯维安®)是首个第三代选择性雌激素受体调节剂(SERM),在欧盟和日本被批准用于治疗绝经后骨质疏松症。巴多昔芬含有一个吲哚为基础的核心结合域,与雌激素受体具有高亲和力,并对骨骼和脂质谱具有有利影响,无临床相关的子宫内膜或乳腺刺激。在一项为期 3 年的大型精心设计的试验中,每日口服巴多昔芬可降低绝经后骨质疏松症患者新发椎体骨折的发生率;巴多昔芬和雷洛昔芬均明显优于安慰剂。在整个研究人群中,巴多昔芬和雷洛昔芬均未降低非椎体骨折的发生率;然而,巴多昔芬而非雷洛昔芬降低了高危患者的非椎体骨折发生率。此外,该试验延长 2 年期间继续接受该药治疗的患者数据表明,巴多昔芬对新椎体骨折的保护作用可长达 5 年。巴多昔芬还可增加骨密度并降低骨转换标志物水平。巴多昔芬在临床试验中通常具有良好的耐受性,不会对生殖道或乳腺组织造成损害,从而显示出有利的风险效益比。一项从欧盟角度进行的药物经济学分析预测,在一些欧盟国家,巴多昔芬具有成本效益。因此,巴多昔芬为绝经后骨质疏松症的治疗提供了另一种有用的选择,特别是对那些骨质疏松性骨折风险较高的患者。