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磷酸雌莫司汀的药代动力学和药效学

Pharmacokinetics and pharmacodynamics of estramustine phosphate.

作者信息

Bergenheim A T, Henriksson R

机构信息

Department of Neurosurgery, Umeå University Hospital, Sweden.

出版信息

Clin Pharmacokinet. 1998 Feb;34(2):163-72. doi: 10.2165/00003088-199834020-00004.

DOI:10.2165/00003088-199834020-00004
PMID:9515186
Abstract

Estramustine phosphate (estramustine phosphate sodium), a carbamate ester combining 17 beta-estradiol and nor-nitrogen mustard, is a cytotoxic drug used in the treatment of advanced prostatic carcinoma. Because of the radiosensitising effect of this drug there has been a recent increase in interest concerning estramustine phosphate and its clinical use. It has also been found that the early recommendations of drug administration together with food or milk were inappropriate, since calcium containing food and antacids hamper drug uptake. This may have obscured results from earlier clinical studies with estramustine phosphate. Estramustine phosphate is currently being re-evaluated for the treatment of other tumours such as glioma and mammary carcinoma. This review summarises the present relatively limited knowledge concerning the pharmacokinetic and pharmacodynamic aspects of estramustine phosphate and its metabolites.

摘要

磷酸雌莫司汀(磷酸雌莫司汀钠)是一种将17β - 雌二醇与去甲氮芥结合的氨基甲酸酯,是一种用于治疗晚期前列腺癌的细胞毒性药物。由于该药物的放射增敏作用,近期人们对磷酸雌莫司汀及其临床应用的兴趣有所增加。还发现早期关于与食物或牛奶一起给药的建议并不恰当,因为含钙食物和抗酸剂会妨碍药物吸收。这可能掩盖了早期磷酸雌莫司汀临床研究的结果。目前正在对磷酸雌莫司汀用于治疗其他肿瘤(如神经胶质瘤和乳腺癌)进行重新评估。本综述总结了目前关于磷酸雌莫司汀及其代谢物的药代动力学和药效学方面相对有限的知识。

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1
Pharmacokinetics and pharmacodynamics of estramustine phosphate.磷酸雌莫司汀的药代动力学和药效学
Clin Pharmacokinet. 1998 Feb;34(2):163-72. doi: 10.2165/00003088-199834020-00004.
2
Synthesis and in vitro evaluation of [carbonyl-11C]estramustine and [carbonyl-11C]estramustine phosphate.
Steroids. 1998 Apr;63(4):228-34. doi: 10.1016/s0039-128x(98)00013-0.
3
Estramustine in malignant glioma.雌莫司汀治疗恶性胶质瘤。
J Neurooncol. 1996 Oct;30(1):81-9. doi: 10.1007/BF00177446.
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Estramustine-binding protein in rat and human prostate.
Scand J Urol Nephrol Suppl. 1988;107:56-8.
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Uptake of estramustine phosphate (estracyt) metabolites in prostatic cancer.磷酸雌莫司汀(癌腺治)代谢物在前列腺癌中的摄取情况。
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Estramustine phosphate (Estracyt): experimental and clinical studies in Europe.磷酸雌莫司汀(癌腺治):欧洲的实验与临床研究
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Uptake and retention of estramustine and the presence of estramustine binding protein in malignant brain tumours in humans.人恶性脑肿瘤中雌莫司汀的摄取与潴留及雌莫司汀结合蛋白的存在情况
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Induction of apoptosis by estramustine phosphate mediated by phosphorylation of bcl-2.磷酸雌莫司汀通过bcl-2磷酸化介导的细胞凋亡诱导作用。
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The Pros and Cons of Estrogens in Prostate Cancer: An Update with a Focus on Phytoestrogens.雌激素在前列腺癌中的利弊:聚焦植物雌激素的最新进展
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本文引用的文献

1
Cytotoxic effect and uptake of estramustine in a rat glioma model.雌莫司汀在大鼠胶质瘤模型中的细胞毒性作用及摄取情况。
Int J Oncol. 1994 Aug;5(2):293-9. doi: 10.3892/ijo.5.2.293.
2
Prognostic implication of estramustine-binding protein in astrocytoma.
Int J Oncol. 1995 Aug;7(2):349-52. doi: 10.3892/ijo.7.2.349.
3
Studies with tritium-labelled hexoestrol in advanced breast cancer. Comparison of tissue accumulation of hexoestrol with response to bilateral adrenalectomy and oophorectomy.氚标记己烷雌酚在晚期乳腺癌中的研究。己烷雌酚的组织蓄积与双侧肾上腺切除术和卵巢切除术反应的比较。
签收、密封、送达:共轭和前药策略作为抗生素的靶向递送载体
ACS Infect Dis. 2019 Jun 14;5(6):816-828. doi: 10.1021/acsinfecdis.9b00019. Epub 2019 Apr 10.
4
Strategies for the Optimization of Natural Leads to Anticancer Drugs or Drug Candidates.优化天然抗癌先导化合物或候选药物的策略。
Med Res Rev. 2016 Jan;36(1):32-91. doi: 10.1002/med.21377. Epub 2015 Sep 11.
5
Identification of secretaglobin Scgb2a1 as a target for developmental reprogramming by BPA in the rat prostate.鉴定分泌球蛋白Scgb2a1为双酚A在大鼠前列腺中进行发育重编程的靶点。
Epigenetics. 2015;10(2):127-34. doi: 10.1080/15592294.2015.1009768.
6
Ribonucleoside 3'-phosphates as pro-moieties for an orally administered drug.核糖核苷3'-磷酸作为口服给药药物的前体部分。
ChemMedChem. 2012 Aug;7(8):1361-4. doi: 10.1002/cmdc.201200243. Epub 2012 Jul 13.
7
Second generation benzofuranone ring substituted noscapine analogs: synthesis and biological evaluation.第二代苯并呋喃酮环取代的纳布啡类似物的合成与生物评价。
Biochem Pharmacol. 2011 Jul 15;82(2):110-21. doi: 10.1016/j.bcp.2011.03.029. Epub 2011 Apr 8.
8
High-grade astrocytoma treated concomitantly with estramustine and radiotherapy.高级别星形细胞瘤同步接受雌莫司汀和放疗治疗。
J Neurooncol. 2006 Jul;78(3):321-6. doi: 10.1007/s11060-005-9106-9. Epub 2006 Apr 6.
9
The bleb formation of the extracellular pseudopodia; early evidence of microtubule depolymerization by estramustine phosphate in glioma cell; in vitro study.细胞外伪足的小泡形成;磷酸雌莫司汀在胶质瘤细胞中导致微管解聚的早期证据;体外研究。
J Neurooncol. 2001 Mar;52(1):37-47. doi: 10.1023/a:1010653613588.
Lancet. 1961 Oct 7;2(7206):796-8. doi: 10.1016/s0140-6736(61)91088-1.
4
Apoptotic tumor cell death induced by estramustine in patients with malignant glioma.
Clin Cancer Res. 1998 Jan;4(1):87-91.
5
Tumor blood flow and the cytotoxic effects of estramustine and its constituents in a rat glioma model.大鼠胶质瘤模型中肿瘤血流以及雌莫司汀及其成分的细胞毒性作用
Neurosurgery. 1997 Jul;41(1):237-43; discussion 243-4. doi: 10.1097/00006123-199707000-00038.
6
Inhibition of prostate cancer growth by estramustine and etoposide: evidence for interaction at the nuclear matrix.
J Urol. 1993 Jun;149(6):1622-5. doi: 10.1016/s0022-5347(17)36463-7.
7
Uptake and retention of estramustine and the presence of estramustine binding protein in malignant brain tumours in humans.人恶性脑肿瘤中雌莫司汀的摄取与潴留及雌莫司汀结合蛋白的存在情况
Br J Cancer. 1993 Feb;67(2):358-61. doi: 10.1038/bjc.1993.65.
8
Estramustine depolymerizes microtubules by binding to tubulin.雌莫司汀通过与微管蛋白结合使微管解聚。
Cancer Res. 1993 Oct 1;53(19):4573-81.
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Estramustine and estrone analogs rapidly and reversibly inhibit deoxyribonucleic acid synthesis and alter morphology in cultured human glioblastoma cells.雌莫司汀和雌酮类似物能迅速且可逆地抑制培养的人胶质母细胞瘤细胞中的脱氧核糖核酸合成并改变其形态。
Neurosurgery. 1993 Mar;32(3):422-30; discussion 430-1. doi: 10.1227/00006123-199303000-00014.
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Estramustine potentiates the effects of irradiation on the Dunning (R3327) rat prostatic adenocarcinoma.雌莫司汀可增强辐射对邓宁(R3327)大鼠前列腺腺癌的作用。
Prostate. 1994;24(2):79-83. doi: 10.1002/pros.2990240205.