磷酸雌莫司汀(Estramustine Phosphate Sodium) - 药物靶点：SHP2_在研适应症：前列腺癌，肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Estramustine 17-(dihydrogen phosphate)、Estramustine Phosphate Sodium Hydrate、Estramustine phosphate sodium (USAN)

+ [11]

靶点

SHP2

作用机制

SHP2抑制剂(蛋白酪氨酸磷酸酶-2抑制剂)、DNA烷化剂

治疗领域

肿瘤泌尿生殖系统疾病

在研适应症

前列腺癌肿瘤

非在研适应症

转移性去势抵抗性前列腺癌

原研机构

Pharmacia & Upjohn, Inc.

在研机构

Pfizer Inc.

Nippon Shinyaku Co., Ltd.Pfizer Italia Srl

+ [1]

非在研机构

Pfizer Canada ULCKabi PharmaciaPharmacia & Upjohn, Inc.

最高研发阶段批准上市

首次获批日期

美国 (1981-12-24),

前列腺癌

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C23H31Cl2NO3

InChIKeyFRPJXPJMRWBBIH-RBRWEJTLSA-N

CAS号2998-57-4

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关联

58

项与磷酸雌莫司汀相关的临床试验

ChiCTR1900023915

/ Suspended临床4期IIT

A prospective, multicenter, randomized, open-lable, controlled study of neoadjuvant chemotherapy with estramustine and radical prostatectomy in patients with high-risk prostate cancer

开始日期2019-07-01

申办/合作机构-

NCT02853071

/ Withdrawn临床2期IIT

Efficacy and Safety of Estracyt® in Metastatic Breast Cancer Hormonal Estrogen Receptor (HER 2) Negative, Hormone Receptor (HR) Positive.

This study evaluates efficacy, safety and quality of life in patients affected by metastatic breast cancer RH+/ HER2- and treated by estramustine phosphate.

开始日期2017-01-01

申办/合作机构

Centre Hospitalier Universitaire de Besancon

NCT02560051

/ Terminated临床2期IIT

Phase 2 Study of Androgen Deprivation Therapy (ADT) Plus Chemotherapy as Initial Treatment for Local Failures or Advanced Prostate Cancer

This study is for men who have prostate cancer and have failed local therapy or are not a candidate for prostatectomy or radiation therapy. The purpose of this research study is to assess the safety and benefit of androgen deprivation therapy (ADT, blocks hormones) plus chemotherapy. Degarelix is the hormone blocking drug that will be used. Doxorubicin, Ketoconazole, Docetaxel and Estramustine are the chemotherapy drugs that will be used. The drugs used in this study are approved by the Food and Drug Administration (FDA).
Participants will be treated with ADT plus chemotherapy for three, four, or five 8-week cycles (12, 18, or 24 months). The number of cycles of chemotherapy they receive and the number of months they receive ADT will be based on their disease. The current standard treatment is ADT and chemotherapy. What differs in this research study is the cycling and combination of chemotherapy drugs chosen. The drugs chosen for this study have fewer side effects and are believed to provide maximum benefit.

开始日期2015-11-01

申办/合作机构

University of Texas Health Science Center at Houston

100 项与磷酸雌莫司汀相关的临床结果

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100 项与磷酸雌莫司汀相关的转化医学

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100 项与磷酸雌莫司汀相关的专利（医药）

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1,089

项与磷酸雌莫司汀相关的文献（医药）

2025-01-01·Anti-Cancer Drugs

Synergistic combination effect of the PCA-1/ALKBH3 inhibitor HUHS015 on prostate cancer drugs in vitro and in vivo

Article

作者: Tsujikawa, Kazutake ; Tanaka, Akito ; Mabuchi, Miyuki

Prostate cancer antigen-1/ALKBH3, a DNA/RNA demethylase of 3-methylcytosine, 1-methyladenine (1-meA), and 6-meA, was found in prostate cancer as an important prognostic factor. Additionally, 1-meA has been associated with other cancers. The ALKBH3 inhibitor HUHS015 was found to be effective against prostate cancer both in vitro and in vivo. Herein, we investigated the effect of HUHS015 in combination with drugs for prostate cancer approved in Japan (including bicalutamide, cisplatin, mitoxantrone, prednisolone, ifosfamide, tegafur/uracil, docetaxel, dacarbazine, and estramustine) by treating DU145 cells with around IC50 value concentrations of these drugs for 3 days. Additionally, the cells were observed for additional 9 days after drug removal. Combination treatment with dacarbazine, estramustine, tegafur/uracil, and HUHS015 showed a slight additive effect after 3 days. After drug washout of them and mitoxantrone, the combined effects and levels were enhanced and sustained, although the effects of each treatment alone declined. HUHS015 combined with cisplatin or docetaxel elicited synergistic and sustained effects. In vivo, combining HUHS015 and docetaxel, the first chemotherapeutic agent for castration-resistant prostate cancer, showed notable effects in the DU145 xenograft model. In conclusion, HUHS015 exhibited a synergistic effect with docetaxel and drugs acting on DNA in vitro, even after drug removal. Since cancer chemotherapy is typically administered during rest periods due to its high toxicity, combining it with an ALKBH3 inhibitor could be a promising strategy for enhancing cancer treatment, as it can elicit an additive effect during treatment, allowing dosage reduction, and synergistically sustain the effect after drug washout during rest periods.

2024-12-01·International Journal of Urology

Dose compliance of estramustine phosphate in neoadjuvant chemohormonal therapy combined with degarelix acetate predicts the biochemical recurrence in patients with very high‐risk prostate cancer who underwent robot‐assisted radical prostatectomy

Article

作者: Murata, Shiori ; Kambe, Takanari ; Yamasaki, Toshinari ; Kokubun, Hidetoshi ; Nagoshi, Akihiko ; Fujiwara, Tasuku ; Hattori, Yuto ; Kawakita, Mutsushi ; Mine, Yuta ; Shibasaki, Noboru ; Akagi, Naoki ; Igarashi, Atsushi ; Yamamoto, Akihiro ; Tsutsumi, Naofumi ; Abe, Yohei ; Hagimoto, Hiroki

ObjectivesThe objective of this study is to evaluate the safety and efficacy of neoadjuvant degarelix acetate and low‐dose estramustine phosphate for high−/very high‐risk prostate cancer.MethodsOverall, 187 patients diagnosed with National Comprehensive Cancer Network high−/very high‐risk cTanyN0M0 localized prostate cancer who consented to undergo robot‐assisted radical prostatectomy after receiving neoadjuvant chemohormonal therapy for 6 months were prospectively enrolled between December 2017 and March 2023. Adverse events, perioperative and histopathological outcomes, and biochemical recurrence‐free survival rates were examined. Survival analysis compared the estramustine phosphate completion and reduction groups.ResultsThirty‐six patients discontinued neoadjuvant therapy in <5 months owing to adverse events (n = 34) or other reasons (n = 2). Eleven were excluded for being in the postoperative castration range. Of the 140 patients who underwent surgery, 124 continued with two tablets of estramustine phosphate and 16 with one tablet. Overall, 82 patients were very high‐risk. Histopathological outcomes were significantly worse in the very high‐risk group than those in the high‐risk group. Very high‐risk status and estramustine phosphate reduction were significant factors in biochemical recurrence in multivariate analysis. The biochemical recurrence‐free survival rate in very high‐risk patients was significantly lower in the estramustine phosphate dose reduction group than in the completion group but not significant in high‐risk patients. Major adverse events were anemia (n = 174), elevated transaminase levels (n = 68), and deep vein thrombosis (n = 24). Severe adverse events included acute coronary syndrome (n = 4) and pulmonary embolism (n = 3).ConclusionsDose compliance with estramustine phosphate predicted biochemical recurrence in patients with very high‐risk prostate cancer undergoing robot‐assisted radical prostatectomy with neoadjuvant chemohormonal therapy.

2024-12-01·Cancer Medicine

Trends in novel antiandrogen receptor signal inhibitor use and medical costs in prostate cancer

Article

作者: Togashi, Kyo ; Ishi, Noritaka ; Okamoto, Teppei ; Hamaya, Tomoko ; Fujita, Naoki ; Yoneyama, Fumiya ; Miura, Hikari ; Oishi, Takuya ; Okuyama, Yoshiharu ; Yamamoto, Hayato ; Ohyama, Chikara ; Tanaka, Ryuma ; Hatakeyama, Shingo

AbstractObjectiveWe aimed to examine trends in novel antiandrogen receptor signal inhibitor (ARSI) usage and medical costs by collecting real‐world big data included in The National Database of Health Insurance Claims and Specific Health Checkups of Japan (NDB) Open Data, covering most of the clinical practices throughout Japan.MethodsUsage data for outpatient prescriptions from 2016 to 2021 were extracted from the NDB Open Data. Among the 459,610 million tablets/capsules prescribed, prostate cancer‐specific agents (bicalutamide, estramustine phosphate, flutamide, abiraterone, enzalutamide, apalutamide, and darolutamide) were selected to investigate the trends of usage and medical costs.ResultsIn total, 764.8 billion medications were recorded. Among these, standard dose‐adjusted prescriptions for bicalutamide, abiraterone, enzalutamide, apalutamide, darolutamide, and other vintages (estramustine phosphate, flutamide) was 276, 14.2, 18.1, 2.19, 0.34, and 20.3 million, respectively. The usage of ARSI increased significantly from 6.1% in 2016 to 16% in 2021. The medical costs for prostate cancer‐specific agents increased significantly (1.8‐fold) from 2016 to 2021. Despite the limited usage of ARSIs, a majority of the medical costs had been spent on ARSIs. Medical costs associated with ARSIs increased significantly from 59% to 89% (p < 0.001).ConclusionARSI usage and medical costs associated with prostate cancer increased significantly from 2016 to 2021. Despite the limited use of ARSIs, a considerable proportion of the medical costs for prostate cancer‐specific agents had been spent on ARSIs.

100 项与磷酸雌莫司汀相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D02398	磷酸雌莫司汀	L01XX11	DB14674

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
前列腺癌	英国	Pfizer Inc.	-

未上市

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适应症	最高研发状态	国家/地区	公司	日期
转移性去势抵抗性前列腺癌	临床2期	美国	Pfizer Inc.	2002-07-01
肿瘤	临床前	美国	H. Lee Moffitt Cancer Center & Research Institute, Inc.	2011-04-15

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00055731 (GETUG-12, ESMO2018) 人工标引	临床3期	前列腺癌	413	goserelin+docetaxel+estramustine	(糧餘構蓋築遞艱壓窪顧) = 醖齋鏇鑰築蓋鏇鏇蓋鹽範積積餘鹽觸夢鬱選艱 (網顧鹽齋壓簾襯網廠衊 ) 更多	积极	2018-10-19
				goserelin	(糧餘構蓋築遞艱壓窪顧) = 繭簾艱鹹鏇製襯範淵膚範積積餘鹽觸夢鬱選艱 (網顧鹽齋壓簾襯網廠衊 ) 更多
NCT02560051 (CTgov)	临床2期	局部晚期前列腺癌 \| 晚期前列腺癌	19	Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Definitive Local Therapy)	鬱構願積網積夢膚繭蓋(願糧餘襯壓範顧繭廠鹹) = 蓋選鹽膚餘壓窪醖醖壓觸膚淵構淵構餘鏇鹽鬱 (膚壓遞築構壓顧網繭醖, 積淵艱艱網構觸積夢齋 ~ 簾衊鑰願鏇願範獵艱範) 更多	-	2018-10-11
				Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Nodal Only/Low-volume Bone)	鬱構願積網積夢膚繭蓋(願糧餘襯壓範顧繭廠鹹) = 襯憲壓觸醖選衊鏇選膚觸膚淵構淵構餘鏇鹽鬱 (膚壓遞築構壓顧網繭醖, 願壓廠蓋獵齋網齋窪鬱 ~ 積襯糧醖餘築鑰艱獵鬱) 更多
NCT00016913 (CTgov)	临床2期	局限性前列腺癌 \| 局部晚期前列腺癌	34	radiation therapy+carboplatin+estramustine+paclitaxel+leuprolide or goserelin acetate	襯範構鬱願鹹遞膚簾膚(糧襯鹹觸鹹選餘艱窪繭) = 製鏇襯壓蓋築廠衊淵艱積壓選壓遞選窪廠鑰網 (構願壓鏇鏇壓鏇遞餘築, 淵廠積製夢襯獵淵簾淵 ~ 膚築窪鏇網蓋夢廠齋鏇) 更多	-	2016-01-29
NCT00055731 (GETUG 12, Pubmed \| Lancet Oncol) 人工标引	临床3期	前列腺癌	413	docetaxel+estramustine+goserelin	(鹹簾襯窪遞網積觸觸製) = 構積繭築餘選鹽遞夢窪齋鏇鏇衊膚餘餘鑰餘淵 (膚廠蓋鹽網夢衊窪鑰鹽 ) 更多	积极	2015-07-01
				goserelin	(鹹簾襯窪遞網積觸觸製) = 積積膚築淵艱鏇鬱廠鑰齋鏇鏇衊膚餘餘鑰餘淵 (膚廠蓋鹽網夢衊窪鑰鹽 ) 更多
NCT00004054 (RTOG-9902, CTgov)	临床3期	局限性前列腺癌	397	Radiation therapy+triptorelin+buserelin+bicalutamide+flutamide+goserelin+leuprolide (Hormones and RT)	(淵鬱窪願壓積鏇膚餘憲) = 範膚遞糧製襯憲襯淵願艱鬱糧選艱遞鑰觸憲鹽 (構夢選醖鹹範壓夢網廠, 願壓顧鬱艱鏇膚繭簾選 ~ 範齋構範鏇壓願築衊廠) 更多	-	2015-01-07
				Radiation therapy+warfarin+etoposide+estramustine phosphate sodium+paclitaxel+bicalutamide+flutamide (Hormones and RT Plus Chemotherapy)	(淵鬱窪願壓積鏇膚餘憲) = 襯醖網構觸衊窪築構築艱鬱糧選艱遞鑰觸憲鹽 (構夢選醖鹹範壓夢網廠, 鹹蓋壓醖鬱襯餘遞鹽廠 ~ 衊壓餘廠窪齋簾壓襯糧) 更多
NCT01250717 (CTgov)	临床2期	局限性前列腺癌	28	Radical Prostatectomy+Estramustine+Docetaxel+Casodex+Dexamethasone+Zoladex	憲膚鹽憲夢衊艱衊艱鏇(醖構網膚廠網憲積構衊) = 憲獵鹹鏇製齋遞範構壓觸製觸選蓋醖淵選選襯 (鏇鏇遞鑰網觸繭襯選製, 遞鹹觸廠鬱餘窪網齋糧 ~ 製蓋憲遞餘觸鹹簾醖鬱) 更多	-	2014-02-04
ASCO_GU2014	N/A	前列腺癌新辅助	-	LHRH agonist/estramustine (Radical Prostatectomy)	(繭夢簾衊獵鹹顧鏇鹹鹽) = 壓築積簾築選網鏇選鬱獵範窪窪鹹襯衊蓋醖鬱 (糧繭淵鹹顧憲襯願憲壓 )	-	2014-02-01
				Radiation Therapy	(繭夢簾衊獵鹹顧鏇鹹鹽) = 鹽壓餘襯膚鏇夢鏇製製獵範窪窪鹹襯衊蓋醖鬱 (糧繭淵鹹顧憲襯願憲壓 )
NCT00028769 (S0032, CTgov)	临床2期	转移性前列腺癌	41	etoposide+estramustine+paclitaxel+bicalutamide+flutamide+leuprolide acetate+goserelin acetate+nilutamide	(鹽醖構衊顧鬱壓網艱範) = 鬱鬱網鑰鑰築廠壓製醖積蓋鹽鹽範鬱衊膚製衊 (構壓膚襯遞夢繭衊醖憲, 鏇積鏇積鬱蓋鬱蓋廠簾 ~ 製築範壓膚艱艱夢糧繭) 更多	-	2013-07-16
HOPLITE (ASCO_GU2012)	临床2期	去势抵抗性前列腺癌一线	148	Continuous Docetaxel (DOC)	遞鬱構蓋蓋鑰餘網築築(獵餘選網鹹繭膚壓蓋繭) = 襯衊夢夢蓋願淵鬱網簾鏇鏇憲衊鹹餘鹹顧廠鑰 (齋築蓋繭顧窪糧膚襯糧 )	不佳	2012-02-10
				Intermittent Docetaxel (DOC)	遞鬱構蓋蓋鑰餘網築築(獵餘選網鹹繭膚壓蓋繭) = 醖遞餘願壓蓋齋範衊憲鏇鏇憲衊鹹餘鹹顧廠鑰 (齋築蓋繭顧窪糧膚襯糧 )
ASCO2011	临床2期	去势抵抗性前列腺癌	-	Cyclophosphamide, etoposide, and estramustine (CEE)	膚獵鏇網願衊糧鏇築膚(襯鹽鹽淵艱醖齋製淵遞) = 構顧餘鏇窪鑰衊憲糧積簾獵繭廠膚鹹鏇網膚積 (鏇醖餘積夢壓窪鹽憲築 ) 更多	-	2011-05-20