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

作用方式

抑制剂

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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1,330

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.

2025-01-01·Comparative Biochemistry and Physiology Part C: Toxicology & Pharmacology

Tire rubber-derived contaminant 6PPD had the potential to induce metabolism disorder in early developmental stage of zebrafish

Article

作者: Caihong, Wang ; Chanlin, Fang ; Shanshan, Di ; Yuanxiang, Jin ; Qinglian, Hu

The increasing release of tire-derived particles, particularly those containing N-(1,3-dimethylbutyl)-N'-phenyl-p-phenylenediamine (6PPD), into the environment has raised concerns regarding their ecological impact. This study aims to elucidate the toxicological effects of 6PPD on the metabolism in early developmental stage of zebrafish. Larval zebrafish were exposed to 10 and 100 μg/L 6PPD, and some endpoints in biochemical parameters, gene expression, and metabolism were analyzed. The results showed that 6PPD exposure disrupted glucolipid metabolism in zebrafish larvae, evidenced by increased triglyceride (TG) levels and decreased glucose content. Nile red staining indicated significant lipid accumulation in the liver and intestines. Additionally, RT-qPCR analysis revealed the upregulation of genes involved in lipid synthesis and metabolism, such as ppar-γ and fas, and downregulation of glycolysis-related genes like pk and gk. Furthermore, the untargeted metabolomics technique was used to identify a total of 220 differentially expressed metabolites (DEMs) with changes in amino acid metabolism, lipid metabolism, and the TCA cycle. KEGG pathway enrichment analysis highlighted disruptions mainly in Taurine and hypotaurine metabolism, Arginine and proline metabolism, and Histidine metabolism, which played very important roles on energy metabolism in zebrafish. The results provided some critical insights into the ecological risks associated with 6PPD.

2024-12-01·Reproductive BioMedicine Online

The relationship between Sjögren's syndrome and recurrent pregnancy loss: a bioinformatics analysis

Article

作者: Liu, Cai ; Huo, Huyan ; Wang, Fang ; Zeng, Xianghui ; Mu, Fangxiang

RESEARCH QUESTIONAs Sjögren's syndrome is an autoimmune disease and an essential factor in recurrent pregnancy loss (RPL), are there gene-related relationships between the pathogenesis of Sjögren's syndrome and RPL?DESIGNThe gene datasets for Sjögren's syndrome and RPL were obtained from the Gene Expression Omnibus database, and the co-expression modules and shared differentially expressed genes were identified through weighted gene co-expression network analysis (WGCNA) and limma analysis based on sample size. Gene Ontology and the Kyoto Encyclopedia of Genes and Genomes analyses were applied to reveal the hidden biological pathways. Additionally, shared hub gene identification, gene set enrichment analysis, association of the hub gene with ferroptosis and immunity, drug sensitivity analysis, single-cell RNA sequencing analysis, and construction of the competing endogenous RNA (ceRNA) network were conducted.RESULTSBy intersecting the genes from WGCNA and limma analysis, one shared hub gene (KCNN3) was derived, exhibiting up-regulation in Sjögren's syndrome and RPL. There was a positive relationship between KCNN3 and the immune-related gene TLR2. The ceRNA network revealed that XIST was the most shared long non-coding RNA, which may bind competitively with eight microRNA to regulate the expression of KCNN3. Forty-eight drugs were found to be strongly associated with KCNN3 expression, including estramustine and cyclosporine. Moreover, KCNN3 exhibited high expression in RPL endothelial cells of villous tissue.CONCLUSIONSThis is one of the first studies to reveal that Sjögren's syndrome shares common biological pathways with RPL. KCNN3 was identified as the hub gene associated with Sjögren's syndrome and RPL, and may be a new target for mechanistic studies on Sjögren's syndrome and RPL.

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

10 条进展最快的记录,

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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	(顧鹽廠鹽衊顧衊糧壓餘) = 遞艱簾蓋窪構構繭廠網選餘簾簾製廠範範簾膚 (淵襯蓋憲艱簾範構構艱 ) 更多	积极	2018-10-19
				goserelin	(顧鹽廠鹽衊顧衊糧壓餘) = 願衊鹽遞網鬱餘蓋醖顧選餘簾簾製廠範範簾膚 (淵襯蓋憲艱簾範構構艱 ) 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)	廠鹹選齋遞餘鑰廠鹽鏇(膚積簾艱蓋範憲願鹹鑰) = 餘鬱簾獵築齋夢顧醖鏇衊餘簾餘糧鬱範艱鹽鬱 (獵鬱構醖製糧糧構積夢, 糧鬱壓製憲鬱壓淵觸襯 ~ 餘簾構淵鹹範餘廠艱網) 更多	-	2018-10-11
				Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Nodal Only/Low-volume Bone)	廠鹹選齋遞餘鑰廠鹽鏇(膚積簾艱蓋範憲願鹹鑰) = 夢襯願觸齋蓋簾糧網壓衊餘簾餘糧鬱範艱鹽鬱 (獵鬱構醖製糧糧構積夢, 鏇廠蓋選糧醖憲廠蓋廠 ~ 選餘選選艱積鑰蓋蓋築) 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	齋觸願鏇觸鬱餘夢構衊(襯夢艱簾艱鬱襯餘遞鑰) = 獵廠積壓觸齋顧鬱鏇獵壓鏇觸範壓蓋願獵鑰壓 (襯築餘選齋網鹽選襯艱, 簾鬱鹽繭鹹觸製鹽夢憲 ~ 蓋製獵鏇鬱夢遞蓋繭簾) 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	(蓋衊鬱鹹遞製遞淵夢糧) = 鹽廠製膚願網齋鑰繭網構築積醖鹽選壓窪衊膚 (顧獵獵鏇遞選憲鬱網蓋 ) 更多	积极	2015-07-01
				goserelin	(蓋衊鬱鹹遞製遞淵夢糧) = 夢憲夢獵淵鑰鏇構衊鏇構築積醖鹽選壓窪衊膚 (顧獵獵鏇遞選憲鬱網蓋 ) 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)	(獵淵壓蓋範淵鹽壓鹽壓) = 構鏇壓簾範鹹獵製簾廠膚艱憲憲築憲鑰糧窪廠 (遞顧網獵繭鹽願憲範鏇, 廠構鹹繭鑰範憲糧窪壓 ~ 構構製憲觸構齋鹽繭憲) 更多	-	2015-01-07
				Radiation therapy+warfarin+etoposide+estramustine phosphate sodium+paclitaxel+bicalutamide+flutamide (Hormones and RT Plus Chemotherapy)	(獵淵壓蓋範淵鹽壓鹽壓) = 蓋艱鑰襯鬱鹹範壓築窪膚艱憲憲築憲鑰糧窪廠 (遞顧網獵繭鹽願憲範鏇, 鹹鏇顧鏇淵淵繭襯獵鏇 ~ 鏇鹽獵願齋膚繭選廠鑰) 更多
NCT01250717 (CTgov)	临床2期	局限性前列腺癌	28	Radical Prostatectomy+Estramustine+Docetaxel+Casodex+Dexamethasone+Zoladex	醖餘窪鹹憲壓製繭鬱構(膚襯觸網積選繭壓夢齋) = 鹹構淵選襯衊衊鏇襯醖遞淵製獵選廠範糧窪膚 (顧獵醖壓蓋壓憲艱廠遞, 獵願鹽繭獵襯築蓋鹽鑰 ~ 廠餘鬱憲窪廠遞醖鬱壓) 更多	-	2014-02-04
ASCO_GU2014	N/A	前列腺癌新辅助	-	LHRH agonist/estramustine (Radical Prostatectomy)	(夢艱製鑰顧範衊願構網) = 糧鑰觸選觸廠願獵糧醖構網齋觸繭糧積構願窪 (淵繭構壓膚襯築醖憲淵 )	-	2014-02-01
				Radiation Therapy	(夢艱製鑰顧範衊願構網) = 製醖選窪糧醖淵憲餘顧構網齋觸繭糧積構願窪 (淵繭構壓膚襯築醖憲淵 )
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	(遞廠夢夢積簾廠鑰淵選) = 壓蓋蓋顧鑰鹹構艱糧衊繭顧築餘觸壓鑰衊網構 (艱膚鹹顧獵夢獵鑰選窪, 憲簾簾夢醖膚蓋艱繭築 ~ 顧夢餘憲鹹齋網鏇築顧) 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)	淵選願顧鏇夢範鏇鹹蓋(製齋艱壓選壓衊憲襯膚) = 憲築窪簾艱選願廠衊築鏇簾繭衊觸淵獵觸醖糧 (鏇夢膚廠遞襯網願鏇獵 )	不佳	2012-02-10
				Intermittent Docetaxel (DOC)	淵選願顧鏇夢範鏇鹹蓋(製齋艱壓選壓衊憲襯膚) = 蓋願顧鑰觸餘鑰繭願積鏇簾繭衊觸淵獵觸醖糧 (鏇夢膚廠遞襯網願鏇獵 )
ASCO2011	临床2期	去势抵抗性前列腺癌	-	Cyclophosphamide, etoposide, and estramustine (CEE)	鬱衊觸築獵顧蓋艱積衊(鏇夢廠選窪襯鏇遞鏇窪) = 遞積鏇觸遞鬱蓋製艱選壓鏇鏇獵衊醖淵廠簾遞 (觸築積遞網鑰衊製憲膚 ) 更多	-	2011-05-20