聚磷酸雌二醇

聚磷酸雌二醇（Polyestradiol phosphate），簡稱PEP，藥品名稱Estradurin，是用來治療男性前列腺癌的雌激素藥品[1][9][2][10]。也可以用來作為治療女性的乳癌、是治療低雌激素症及更年期症狀的激素替代療法藥物之一，也是給跨性別女性的女性化賀爾蒙治療[1][11]，以每4個星期一次肌肉注射的方式給藥[1][2][12]。

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聚磷酸雌二醇
上圖：聚磷酸雌二醇的键线式，下圖：雌二醇磷酸酯（聚磷酸雌二醇的单体）的球棒模型
臨床資料
商品名Estradurin, Estradurine
其他名稱PEP; Estradiol phosphate polymer; Estradiol 17β-phosphate polymer; Estradiol polymer with phosphoric acid; Leo-114
AHFS/Drugs.com国际药品名称
懷孕分級
给药途径肌肉注射[1][2]
藥物類別雌激素藥物、雌激素酯
ATC碼
法律規範狀態
法律規範
  • 处方药（℞-only）
藥物動力學數據
生物利用度肌肉注射: 高
血漿蛋白結合率雌二醇：~98%（和albumin及SHBG）[3][4][1]
药物代谢主要是靠肝臟，少部份會透過腎、生殖腺及肌肉（透過磷酸酶）[1]
代謝產物雌激素藥物、磷酸及雌激素的代謝產物[5][6]
生物半衰期PEP: 70 days (10 weeks)[7]
Estradiol: 1–2 hours[8]
排泄途徑尿）（依生物轉化作用）[1]
识别
  • Estra-1,3,5(10)-triene-3,17β-diol, polymer with phosphoric acid
CAS号28014-46-2  checkY
PubChem SID
DrugBank
ChemSpider
  • None
UNII
KEGG
ChEMBL
化学
化学式(C18H23O4P)n
(n = variable; n = 13)
摩尔质量聚合物: 不固定
重覆單元: 334.347 g/mol
熔点195至202 °C（383至396 °F）

参考文献
  1. . [2018-01-01]. （原始内容存档于2018-01-02）.
  2. Mikkola A, Ruutu M, Aro J, Rannikko S, Salo J. . Ann Chir Gynaecol. 1999, 88 (1): 18–21. ISSN 0355-9521. PMID 10230677. Orchiectomy and estrogens have been used for over 50 years in the treatment of advanced prostatic cancer. Although orchiectomy is a simple procedure, it may cause psychological stress. Oral estrogen therapy is as effective as orchiectomy in terms of cancer inhibitory effect, but its acceptance as primary hormonal treatment is overshadowed by an increased risk of cardiovascular complications. Parenteral estrogen, polyestradiol phosphate (PEP), is effective, but also associated with cardiovascular complications, although to a lesser extent. During the last 20 years, well tolerated luteinizing hormone releasing hormone (LHRH) analogues have been replacing orchiectomy and estrogens. Efforts have been made to increase the efficacy of the treatment by adding antiandrogens to LHRH analogues and also to orchiectomy (combined androgen blockade, CAB). However, the efficacy of LHRH analogues and CAB has not proved to be superior to that of simple orchiectomy and, moreover, they are expensive treatment modalities. Orchiectomy and LHRH analogues are associated with negative effects on bone mass and may cause osteoporosis, whereas PEP treatment has an opposite effect. Parenteral polyestradiol phosphate is still a cheap potential treatment for advanced prostatic cancer, but further studies should be conducted to establish its future role, e.g. combining acetylsalicylic acid to prevent cardiovascular complications.
  3. Stanczyk, Frank Z.; Archer, David F.; Bhavnani, Bhagu R. . Contraception. 2013, 87 (6): 706–727. ISSN 0010-7824. PMID 23375353. doi:10.1016/j.contraception.2012.12.011.
  4. Tommaso Falcone; William W. Hurd. . Elsevier Health Sciences. 2007: 22,362,388 [2021-01-26]. ISBN 978-0-323-03309-1. （原始内容存档于2021-04-15）.
  5. Michael Oettel; Ekkehard Schillinger. . Springer Science & Business Media. 6 December 2012: 261,544 [2021-01-26]. ISBN 978-3-642-60107-1. （原始内容存档于2021-03-07）. Natural estrogens considered here include: [...] Esters of 17β-estradiol, such as estradiol valerate, estradiol benzoate and estradiol cypionate. Esterification aims at either better absorption after oral administration or a sustained release from the depot after intramuscular administration. During absorption, the esters are cleaved by endogenous esterases and the pharmacologically active 17β-estradiol is released; therefore, the esters are considered as natural estrogens.
  6. Kuhl H. (PDF). Climacteric. 2005,. 8 Suppl 1: 3–63 [2021-01-26]. PMID 16112947. S2CID 24616324. doi:10.1080/13697130500148875. （原始内容 (PDF)存档于2016-08-22）.
  7. Stege R, Gunnarsson PO, Johansson CJ, Olsson P, Pousette A, Carlström K. . Prostate. May 1996, 28 (5): 307–10. PMID 8610057. doi:10.1002/(SICI)1097-0045(199605)28:5<307::AID-PROS6>3.0.CO;2-8.
  8. Düsterberg B, Nishino Y. . Maturitas. 1982, 4 (4): 315–24. PMID 7169965. doi:10.1016/0378-5122(82)90064-0.
  9. Stege R, Carlström K, Hedlund PO, Pousette A, von Schoultz B, Henriksson P. [Intramuscular depot estrogens (Estradurin) in treatment of patients with prostate carcinoma. Historical aspects, mechanism of action, results and current clinical status]. Urologe A. September 1995, 34 (5): 398–403. ISSN 0340-2592. PMID 7483157 （德语）. More than 50 years ago, orally given estrogen was already used in the treatment of prostate cancer. Due to cardiovascular side-effects with a high morbidity of 25%, this treatment has not become standard. Recent investigations show that parenteral application reduces the risk of cardiovascular side-effects, because it avoids the first passage through the liver with high concentrations of estrogen which normally occur after oral application. Therefore, an increased synthesis of so-called "steroid-sensitive" liver proteins, such as coagulation factors (especially factor VII) can be avoided. This newer parenteral estrogen application shows encouraging results of a cheap and effective hormonal therapy with a low rate of side-effects in patients with prostate cancer.
  10. Mikkola, A; Aro, J; Rannikko, S; Ruutu, M; Finnprostate, Group. . Prostate. March 2007, 67 (4): 447–55. PMID 17219379. S2CID 20549248. doi:10.1002/pros.20547.
  11. Urdl, W. [Therapeutic principles in transsexualism]. Gynäkologische Endokrinologie. 2009, 7 (3): 153–160. ISSN 1610-2894. S2CID 8001811. doi:10.1007/s10304-009-0314-9 （德语）.
  12. Steinbach T, Wurm FR. . Angew. Chem. Int. Ed. Engl. 2015, 54 (21): 6098–108. PMID 25951459. doi:10.1002/anie.201500147.
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