用戶:江舟孤雪/草擬之書
雷洛昔芬
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| 臨床資料 | |
|---|---|
| 核准狀況 | |
| 懷孕分級 |
|
| 給藥途徑 | 口服 |
| ATC碼 | |
| 法律規範狀態 | |
| 法律規範 |
|
| 藥物動力學數據 | |
| 生物利用度 | 2% |
| 血漿蛋白結合率 | 95% |
| 藥物代謝 | 肝的葡糖苷酸結合物 |
| 生物半衰期 | 27.7 小時 |
| 排泄途徑 | 糞便 |
| 識別資訊 | |
| |
| CAS號 | 84449-90-1 |
| PubChem CID | |
| DrugBank | |
| 化學資訊 | |
| 化學式 | C28H27NO4S |
| 摩爾質量 | 473.584 g/mol |
| 3D模型（JSmol） | |
| |
雷洛昔芬 是口服的選擇性雌激素受體調節劑 (SERM)，對骨質有雌激素作用而對子宮和乳房有抗雌激素作用。該藥用於預防絕經後婦女的骨質疏鬆症。2006年4月17日，有研究指出雷洛昔芬對減少高危女性乳腺癌的發病率與他莫昔芬效果相同，[1]而且對於服用雷洛昔芬的患者還比服用他莫昔芬的減少了患血栓栓塞問題和白內障的風險。[1]2007年9月14日，美國FDA宣佈批准雷洛昔芬用於預防和治療骨質疏鬆和降低乳腺癌的風險。[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.[來源請求]
雷洛昔芬是由禮來公司開發，以Evista為商品名銷售。
性狀
[編輯]鹽酸雷洛昔芬的化學式為C28H27NO4S•HCl，分子量為510.05 g/mol。鹽酸雷洛昔芬是白色或淺黃色微溶於水的固體。
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
[編輯]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
[編輯]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
[編輯]Common adverse events considered to be drug-related were hot flashes and leg cramps.[來源請求]
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
[編輯]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
[編輯]- ^ 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 (新聞稿). 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
[編輯]- 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 美國國家女性健康網(National Women's Health Network)的意見書
{{Sex hormones}} [[Category:Benzothiophenes]] [[Category:Eli Lilly and Company]] [[Category:Piperidines]] [[Category:Selective estrogen receptor modulators]] [[de:Raloxifen]] [[en:Raloxifene]] [[it:Raloxifene]] [[hu:Raloxifen]]