Delving into the Latest Updates on Estramustine Phosphate Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

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

+ [11]

Target

SHP2

Mechanism

SHP2 inhibitors(Src homology phosphotyrosyl phosphatase 2 inhibitors), DNA alkylating agents

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Prostatic CancerNeoplasms

Inactive Indication

Metastatic castration-resistant prostate cancer

Originator Organization

Pharmacia & Upjohn, Inc.

Active Organization

Pfizer Inc.

Nippon Shinyaku Co., Ltd.Pfizer Italia Srl

+ [1]

Inactive Organization

Pfizer Canada ULCKabi PharmaciaPharmacia & Upjohn, Inc.

Drug Highest PhaseApproved

First Approval Date

US (24 Dec 1981),

Prostatic Cancer

Regulation-

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Structure

Molecular FormulaC23H31Cl2NO3

InChIKeyFRPJXPJMRWBBIH-RBRWEJTLSA-N

CAS Registry2998-57-4

View All Structures (2)

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.

Start Date01 Nov 2015

Sponsor / Collaborator

University of Texas Health Science Center at Houston

NCT02494713 / TerminatedPhase 2IIT

Neoadjuvant Androgen Deprivation Therapy and Chemotherapy Followed by Radical Prostatectomy in Patients With Prostate Cancer

This is a study for men who have locally-advanced prostate cancer and are eligible to undergo prostatectomy. Standard treatment is prostatectomy alone, but there is a chance that cancer may spread to other organs in the future, even after the prostate is removed. If this were to occur, standard treatment would be androgen deprivation therapy (ADT; hormone therapy that blocks testosterone) plus chemotherapy. Clinical trials suggest that neoadjuvant treatment (treatment given before primary therapy) may prevent a recurrence. The purpose of this research study is to assess the safety and benefit of ADT plus chemotherapy given before prostate removal.

Start Date01 Oct 2015

Sponsor / Collaborator

University of Texas Health Science Center at Houston

EUCTR2010-021962-31-SE / Unknown statusNot ApplicableIIT

KEES- A single arm phase II trial of the peroral regimen KEES (Ketokonazole, Etoposide, Estramustine, Sendoxan) in patients with Castration Resistant Prostate Cancer (CRPC) - KEES- a phase II study in patients with CRPC

Start Date06 Oct 2011

Sponsor / Collaborator-

100 Clinical Results associated with Estramustine Phosphate Sodium

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100 Translational Medicine associated with Estramustine Phosphate Sodium

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100 Patents (Medical) associated with Estramustine Phosphate Sodium

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1,067

Literatures (Medical) associated with Estramustine Phosphate Sodium

01 Dec 2024·Reproductive BioMedicine Online

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

Article

Author: Liu, Cai ; Wang, Fang ; Huo, Huyan ; 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.

10 Sep 2024·International journal of urology : official journal of the Japanese Urological Association

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

Author: Murata, Shiori ; Kambe, Takanari ; Yamasaki, Toshinari ; Kokubun, Hidetoshi ; Nagoshi, Akihiko ; Fujiwara, Tasuku ; Kawakita, Mutsushi ; Hattori, Yuto ; 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.

01 Jul 2024·European Urology Focus

Radiation Therapy for Locally Advanced Prostate Cancer: How Do We Treat Patients with cN1 Disease?

Review

Author: Hyafil, Fabien ; Oudard, Stéphane ; Arnaud, Méjean ; Bibault, Jean-Emmanuel ; Thibault, Constance

Radiotherapy (RT) for high-risk localized prostate cancer (HRLPC) can be controversial in the context of increasing detection of suspicious lymph nodes via advanced imaging techniques. The EORTC 22683 trial initially established RT with androgen deprivation therapy (ADT) as the standard of care for HRLPC, but many patients remain uncured. GETUG-AFU-12 showed that addition of docetaxel and estramustine to ADT improved relapse-free survival but not overall survival. STAMPEDE later demonstrated that abiraterone acetate with ADT and RT significantly improved failure-free survival and overall survival. Ongoing trials such as ENZARAD, ATLAS, DASL-HiCap, and GETUG-P17 ALADDIN are investigating the efficacy of new androgen receptor pathway inhibitors combined with RT and ADT. These studies aim to refine treatment strategies for HRLPC, particularly in the context of advanced imaging and patient upstaging. PATIENT SUMMARY: Addition of newer medications to standard radiation therapy has shown promise in improving survival for men with high-risk prostate cancer. Ongoing studies are testing these options to find the best combination. The aim is to increase the chances of curing prostate cancer, especially as advanced scan techniques are detecting more cases.

100 Deals associated with Estramustine Phosphate Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
D02398	Estramustine Phosphate Sodium	L01XX11	DB14674

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Prostatic Cancer	GB	Pfizer Inc.	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Metastatic castration-resistant prostate cancer	Phase 1	US	Pfizer Inc.	01 Jul 2002
Neoplasms	Preclinical	US	H. Lee Moffitt Cancer Center & Research Institute, Inc.	15 Apr 2011

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00055731 (GETUG-12, ESMO2018) Manual	Phase 3	Prostatic Cancer	413	goserelin+docetaxel+estramustine	(dxpidyqhlq) = mjwfrgrrpf odmgwlpsqj (ltkmmalnwi ) View more	Positive	19 Oct 2018
				goserelin	(dxpidyqhlq) = krohuiwelb odmgwlpsqj (ltkmmalnwi ) View more
NCT02560051 (CTgov)	Phase 2	Locally Advanced Prostate Carcinoma \| Advanced Prostate Carcinoma	19	Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Definitive Local Therapy)	bqcanoikrg(tmugbkhlty) = dspovokafj ofjeftbxta (jcdycunfqo, aflpkaiepo - xptxumgllc) View more	-	11 Oct 2018
				Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Nodal Only/Low-volume Bone)	bqcanoikrg(tmugbkhlty) = usatovrzaq ofjeftbxta (jcdycunfqo, vfblyqltdr - imnwvumfsr) View more
NCT00055731 (GETUG 12, Pubmed \| Lancet Oncol) Manual	Phase 3	Prostatic Cancer	413	docetaxel+estramustine+goserelin	(jxkqiazopj) = hlybcqcfwx zoluxojrnj (szxsxyeuut ) View more	Positive	01 Jul 2015
				goserelin	(jxkqiazopj) = axfqoytdmq zoluxojrnj (szxsxyeuut ) View more
NCT00004054 (RTOG-9902, CTgov)	Phase 3	Localized Prostate Carcinoma	397	Radiation therapy+triptorelin+buserelin+bicalutamide+flutamide+goserelin+leuprolide (Hormones and RT)	gpmmhmdalx(pmywsgthtk) = sxtvgioqkx htorwjmzqt (pfggyjutya, kwwekomekj - jmoftmrizn) View more	-	07 Jan 2015
				Radiation therapy+warfarin+etoposide+estramustine phosphate sodium+paclitaxel+bicalutamide+flutamide (Hormones and RT Plus Chemotherapy)	gpmmhmdalx(pmywsgthtk) = asybkzkgit htorwjmzqt (pfggyjutya, wgclalrudc - bxesmddvwb) View more
ASCO_GU2014	Not Applicable	Prostatic Cancer Neoadjuvant	-	LHRH agonist/estramustine (Radical Prostatectomy)	(vnzyxqmqdk) = ekfvxtrjhe ysjxcangiu (pofycugbjr )	-	01 Feb 2014
				Radiation Therapy	(vnzyxqmqdk) = ahlsfpgcbo ysjxcangiu (pofycugbjr )
HOPLITE (ASCO_GU2012)	Phase 2	Castration-Resistant Prostatic Cancer First line	148	Continuous Docetaxel (DOC)	mblarnfyrp(iuwvujftut) = kasvaftesy avepyfjllg (getpvcebjj )	Negative	10 Feb 2012
				Intermittent Docetaxel (DOC)	mblarnfyrp(iuwvujftut) = yjazzjobio avepyfjllg (getpvcebjj )
ASCO2011	Phase 2	Castration-Resistant Prostatic Cancer	-	Cyclophosphamide, etoposide,Cyclophosphamide, etoposide, and estramustine (CEE)	gnamnmtruy(rxphdixuoo) = iubrwgehtf ajqomyfxcy (aeedtpxrxm ) View more	-	20 May 2011
NCT00052845 (Cancer and leukemia group B trial 90004, Pubmed \| Clin Genitourin Cancer)	Phase 2	Castration-Resistant Prostatic Cancer	80	Estramustine	mvtfbvubkn(vkaaonyysw) = The combination of estramustine/docetaxel/exisulind was associated with significant thomboembolic toxicity despite prophylactic warfarin cqlfrealhw (ocsljdhamo )	-	01 Sep 2008
ASCO2008	Phase 2	Metastatic castration-resistant prostate cancer	60	Estramustine, paclitaxel, and tegafur-uracil (ETU)	qquaixtfqw(jehcgieioi) = 36% of patients gpnwajyzae (ezeagoqdda ) View more	-	20 May 2008
ASCO2008	Phase 1/2	Solid tumor First line	22	Docetaxel	(ayngnmakdn) = jlbcjmwkla zamtmuvuga (mizfyrznfy )	-	20 May 2008
				Irinotecan	(ayngnmakdn) = oammsafzin zamtmuvuga (mizfyrznfy )