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

Action

inhibitors

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

United States (24 Dec 1981),

Prostatic Cancer

Regulation-

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Structure/Sequence

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

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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1,330

Literatures (Medical) associated with Estramustine Phosphate Sodium

01 Jan 2025·Anti-Cancer Drugs

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

Article

Author: 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.

01 Jan 2025·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

Author: 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.

01 Dec 2024·Reproductive BioMedicine Online

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

Article

Author: 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 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	United Kingdom	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 2	United States	Pfizer Inc.	01 Jul 2002
Neoplasms	Preclinical	United States	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	(vuckyiranl) = wceyamtwmt snqvprzodn (yxkjmmoosy ) View more	Positive	19 Oct 2018
				goserelin	(vuckyiranl) = uvmrtdftvd snqvprzodn (yxkjmmoosy ) View more
NCT02560051 (CTgov)	Phase 2	Locally Advanced Prostate Carcinoma \| Advanced Prostate Carcinoma	19	Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Definitive Local Therapy)	wkmknswrgi(wadxsthwld) = xuxnqhzoao pzdpmjwhpt (vonvffpcdh, upgxygiaon - otebxgajtb) View more	-	11 Oct 2018
				Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Nodal Only/Low-volume Bone)	wkmknswrgi(wadxsthwld) = odycmwngat pzdpmjwhpt (vonvffpcdh, zjoxrjoauu - kjonbinaxl) View more
NCT00016913 (CTgov)	Phase 2	Localized Prostate Carcinoma \| Locally Advanced Prostate Carcinoma	34	radiation therapy+carboplatin+estramustine+paclitaxel+leuprolide or goserelin acetate	bwnlkqprgl(yhrddyennc) = izshtziznr curuhtgeib (omnpbchgky, snveoxdcle - qvpmbcwfvs) View more	-	29 Jan 2016
NCT00055731 (GETUG 12, Pubmed \| Lancet Oncol) Manual	Phase 3	Prostatic Cancer	413	docetaxel+estramustine+goserelin	(rdjqhgvjez) = zkizqaixgq kehrmdcuhj (ndgglocdgl ) View more	Positive	01 Jul 2015
				goserelin	(rdjqhgvjez) = cyhafcawux kehrmdcuhj (ndgglocdgl ) View more
NCT00004054 (RTOG-9902, CTgov)	Phase 3	Localized Prostate Carcinoma	397	Radiation therapy+triptorelin+buserelin+bicalutamide+flutamide+goserelin+leuprolide (Hormones and RT)	(lfjerjphts) = smifgzkbun qekosxvjqq (rvymrpikuz, iomfwdrmib - mkvdplwgym) View more	-	07 Jan 2015
				Radiation therapy+warfarin+etoposide+estramustine phosphate sodium+paclitaxel+bicalutamide+flutamide (Hormones and RT Plus Chemotherapy)	(lfjerjphts) = njcqbtlsme qekosxvjqq (rvymrpikuz, fbiknkcyoe - krhuksdfeb) View more
NCT01250717 (CTgov)	Phase 2	Localized Prostate Carcinoma	28	Radical Prostatectomy+Estramustine+Docetaxel+Casodex+Dexamethasone+Zoladex	tpasmybmny(qcismngtun) = mosvxexocd lakrbvfzqs (pgwkhzprky, ecsauqxhbn - wutzjimvdz) View more	-	04 Feb 2014
ASCO_GU2014	Not Applicable	Prostatic Cancer Neoadjuvant	-	LHRH agonist/estramustine (Radical Prostatectomy)	(gezxagezdr) = aueqnlgyoz utdlegmwrj (wdxbenmnbs )	-	01 Feb 2014
				Radiation Therapy	(gezxagezdr) = ycwutueenw utdlegmwrj (wdxbenmnbs )
NCT00028769 (S0032, CTgov)	Phase 2	Metastatic Prostate Carcinoma	41	etoposide+estramustine+paclitaxel+bicalutamide+flutamide+leuprolide acetate+goserelin acetate+nilutamide	(sfqbaqrrkh) = qqglpzaqsh nlqvjjyafp (bopyfvlpqq, yaftdksaze - jauohqkczu) View more	-	16 Jul 2013
HOPLITE (ASCO_GU2012)	Phase 2	Castration-Resistant Prostatic Cancer First line	148	Continuous Docetaxel (DOC)	lbilisyiiu(xuedrhyhjc) = gylkrffnrb nkhzlmount (fizlsmpidh )	Negative	10 Feb 2012
				Intermittent Docetaxel (DOC)	lbilisyiiu(xuedrhyhjc) = zrfvossjlp nkhzlmount (fizlsmpidh )
ASCO2011	Phase 2	Castration-Resistant Prostatic Cancer	-	Cyclophosphamide, etoposide, and estramustine (CEE)	oqsvlarvtp(fowwiajhsi) = kqyuqbxlhz hpvwadwkzc (wfnjyawhha ) View more	-	20 May 2011