用户:江舟孤雪/草拟之书
雷洛昔芬
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| 临床资料 | |
|---|---|
| 核准状况 | |
| 怀孕分级 |
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| 给药途径 | 口服 |
| ATC码 | |
| 法律规范状态 | |
| 法律规范 |
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| 药物动力学数据 | |
| 生物利用度 | 2% |
| 血浆蛋白结合率 | 95% |
| 药物代谢 | 肝的葡糖苷酸结合物 |
| 生物半衰期 | 27.7 小时 |
| 排泄途径 | 粪便 |
| 识别信息 | |
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| CAS号 | 84449-90-1 |
| PubChem CID | |
| DrugBank | |
| 化学信息 | |
| 化学式 | C28H27NO4S |
| 摩尔质量 | 473.584 g/mol |
| 3D模型（JSmol） | |
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雷洛昔芬 是口服的选择性雌激素受体调节剂 (SERM)，对骨质有雌激素作用而对子宫和乳房有抗雌激素作用。该药用于预防绝经后妇女的骨质疏松症。2006年4月17日，有研究指出雷洛昔芬对减少高危女性乳腺癌的发病率与他莫昔芬效果相同，[1]而且对于服用雷洛昔芬的患者还比服用他莫昔芬的减少了患血栓栓塞问题和白内障的风险。[1]2007年9月14日，美国FDA宣布批准雷洛昔芬用于预防和治疗骨质疏松和降低乳腺癌的风险。[2]
There has been criticism in the mainstream oncology press of the way that information about the drug was released.[3] There has been some confusion in the lay media about the meaning of the trial results. There is no specific clinical evidence for the use of raloxifene in the adjuvant treatment of breast cancer over established drugs such as tamoxifen or anastrozole.[来源请求]
雷洛昔芬是由礼来公司开发，以Evista为商品名销售。
性状
[编辑]盐酸雷洛昔芬的化学式为C28H27NO4S•HCl，分子量为510.05 g/mol。盐酸雷洛昔芬是白色或浅黄色微溶于水的固体。
SERMs mimic estrogen in some tissues and have anti-estrogen activity in others. Other SERMs, such as Pfizer's lasofoxifene and Wyeth's bazedoxifene are in the later [... finish the sentence ...]
Indication
[编辑]Raloxifene is indicated for the treatment and prevention of osteoporosis in postmenopausal women, for reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. For either osteoporosis treatment or prevention, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate.
Contraindications and precautions
[编辑]Raloxifene is contraindicated in lactating women or women who are or may become pregnant, in women with active or past history of venous thromboembolic events, including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis and in women known to be hypersensitive to raloxifene.
Adverse reactions
[编辑]Common adverse events considered to be drug-related were hot flashes and leg cramps.[来源请求]
Raloxifene may infrequently cause serious blood clots to form in the legs, lungs, or eyes. Other reactions experienced include leg swelling/pain, trouble breathing, chest pain, vision changes.Raloxifene is a teratogenic drug.
In a 2006 study published in New England Journal of Medicine, raloxifene produced significantly more strokes and blood clots than the placebo.[2]
As cancer drug
[编辑]Raloxifene reduces the risk of hormone-positive breast cancer and vertebral fractures "without a shadow of a doubt," but its effects on cardiovascular disease remain less certain, according to the results of the "Raloxifene for Use of the Heart" (RUTH) study published in the July 13, 2006 issue of the New England Journal of Medicine by Dr. Elizabeth Barrett-Connor (University of California at San Diego) and colleagues.[4]
In the trial, in women with coronary heart disease (CHD) or multiple risk factors for CHD, raloxifene had no significant effect on the primary end point, coronary events, but it did significantly increase the risk of venous thromboembolism (VTE). And although the drug had no effect on stroke, there was a seemingly paradoxical significant increase in death from stroke.[5]
On September 14, 2007, Steven K. Galson, then director of the United States Food and Drug Administration's Center for Drug Evaluation and Research announced authorization of the sale of raloxifene to prevent invasive breast cancer in post-menopausal women.[6]
References
[编辑]- ^ Vogel, Victor; Joseph Constantino, Lawrence Wickerman et al.. Effects of Tamoxifen vs. Raloxifene on the Risk of Developing Invasive Breast Cancer and Other Disease Outcomes. The Journal of the American Medical Association. 2006, 295 (23): 2727–2741. PMID 16754727. doi:10.1001/jama.295.23.joc60074.
- ^ FDA Approves New Uses for Evista (新闻稿). U.S. Food and Drug Administration. 2007-09-14 [2007-09-15].
- ^ Thelancetoncology,. A STARring role for raloxifene?. Lancet Oncol. 2006, 7 (6): 443. PMID 16750489. doi:10.1016/S1470-2045(06)70701-X.
- ^ Lisa Nainggolan. A balancing act: The pro and cons of raloxefene. July 12, 2006.
- ^ Barrett-Connor E, Mosca L, Collins P; et al. Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women. New England Journal of Medicine. 2006, 355: 125–137. PMID 16837676. doi:10.1056/NEJMoa062462.
- ^ AFP.google.com, US approves Lilly's Evista for breast cancer prevention
- Heringa M. Review on raloxifene: profile of a selective estrogen receptor modulator. Int J Clin Pharmacol Ther. 2003, 41 (8): 331–45. PMID 12940590.
- Barrett-Connor E. Raloxifene: risks and benefits. Ann N Y Acad Sci: 295–303. PMID 11795366.
External links
[编辑]- STAR: a head-to-head comparison of tamoxifen and raloxifene as breast-cancer preventatives
- Full Prescribing Information
- [http://www.nwhn.org/publications/position_details.php?poid=5 美国国家女性健康网(National Women's Health Network)的意见书
{{Sex hormones}} [[Category:Benzothiophenes]] [[Category:Eli Lilly and Company]] [[Category:Piperidines]] [[Category:Selective estrogen receptor modulators]] [[de:Raloxifen]] [[en:Raloxifene]] [[it:Raloxifene]] [[hu:Raloxifen]]