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 (USAN), Estramustine Phosphate Sodium Hydrate

+ [8]

Target-

Mechanism

DNA alkylating agents

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication

Prostatic Cancer

Inactive Indication

Adenocarcinoma of prostateCastration-Resistant Prostatic CancerLocalized Prostate Carcinoma+ [3]

Originator Organization

Pharmacia & Upjohn, Inc.

Active Organization

Nippon Shinyaku Co., Ltd.

Pfizer Inc.Pfizer Italia Srl

+ [1]

Inactive Organization

The University of Texas MD Anderson Cancer CenterPfizer Canada ULCKabi Pharmacia

+ [3]

Drug Highest PhaseApproved

First Approval Date

US (24 Dec 1981),

Prostatic Cancer

Regulation-

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Structure

Molecular FormulaC23H32Cl2NNa2O6P

InChIKeyIVXNINGCQWCJJG-VVSKJQCTSA-N

CAS Registry52205-73-9

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 Applicable

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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1,050

Literatures (Medical) associated with Estramustine Phosphate Sodium

01 Oct 2023·Clinical genitourinary cancer

Very Long-Term Complete Remission Can Be Achieved in Men With High-Risk Localized Prostate Cancer and a Very High PSA Value: An Analysis of the GETUG 12 Phase 3 Trial.

Article

Author: Legouffe, Eric ; Grosse-Goupil, Marine ; Culine, Stéphane ; Fléchon, Aude ; Krakowski, Ivan ; Lagrange, Jean-Léon ; Brihoum, Meryem ; Theodore, Christine ; Rolland, Frédéric ; Davin, Jean-Louis ; Berdah, Jean-François ; Labourey, Jean-Luc ; Beuzeboc, Philippe ; Deplanque, Gaël ; Lesaunier, François ; Oudard, Stéphane ; Teuff, Gwénaël Le ; Laguerre, Brigitte ; Martin, Anne-Laure ; Fizazi, Karim ; Ferrero, Jean-Marc ; Drubay, Damien ; Orlando, Valentina ; Cojean-Zelek, Isabelle ; Lavaud, Pernelle ; Houede, Nadine ; Faivre, Laura ; Baciuchka, Marjorie ; Delva, Remy ; Linassier, Claude ; Priou, Frank ; Chinet-Charrot, Paule ; Gravis, Gwenaëlle ; Mourey, Loic

INTRODUCTION:

Serum prostate specific antigen (PSA) is a well-known prognostic parameter in men with prostate cancer. The treatment of men with very high PSA values and apparently no detectable metastases is not fully established.

PATIENTS AND METHODS:

Ancillary analysis from the GETUG 12 phase 3 trial. Patients with non-metastatic high-risk prostate cancer by bone and computerized tomography (CT) scan were randomly assigned to receive androgen deprivation therapy (ADT) and docetaxel plus estramustine or ADT alone. Relapse-free survival (RFS), clinical RFS, metastases-free survival (MFS), overall survival (OS), and prostate cancer-specific survival (PCSS) were estimated using the Kaplan-Meier method for different levels of PSA (50 ng/mL, 75 ng/mL, and 100 ng/mL). The relationship between PSA and outcomes was studied using residual-based approaches and spline functions.

RESULTS:

The median follow-up was 12 years (range: 0-15.3). Baseline PSA (<50 ng/mL, n = 328; ≥50ng/mL, n = 85) was associated with improved RFS (P = .0005), cRFS (P = .0024), and MFS (P = .0068). The 12-year RFS rate was 46.33% (CI 40.59-51.86), 33.59% (CI 22.55-44.97), and 11.76% (1.96-31.20) in men with PSA values <50 ng/mL (n = 328), 50-100 ng/mL (n = 68), and ≥100 ng/mL (n = 17), respectively. Exploratory analyses revealed no deviation from the linear relationship assumption between PSA and the log hazard of events.

CONCLUSIONS:

Men with apparently localized prostate cancer and a high baseline PSA value have a reasonable chance of being long-term disease-free when treated with curative intent combining systemic and local therapy.

Journal of materials chemistry. B

Theranostic inorganic–organic hybrid nanoparticles with a cocktail of chemotherapeutic and cytostatic drugs

Article

Author: Napp, Joanna ; Feldmann, Claus ; Schepers, Ute ; Khorenko, Mikhail ; Meschkov, Anna ; Alves, Frauke ; Pfeifer, Juliana

Theranostic inorganic–organic hybrid nanoparticles (IOH-NPs) with a cocktail of chemotherapeutic and cytostatic drugs and outstanding drug loading (71–82% of total nanoparticle mass) are evaluated with different cell lines and tumor spheroids.

04 Apr 2023·BMC cancer

Activity and safety of KEES - an oral multi-drug chemo-hormonal metronomic combination regimen in metastatic castration-resistant prostate cancer.

Article

Author: Papantoniou, Dimitrios ; Ekholm, Maria ; Asowed, Mustafa ; Elander, Nils O ; Pettersson, Linn

BACKGROUND:

Metastatic castration-resistant prostate cancer (mCRPC) remains a therapeutic challenge and evidence for late-line treatments in real-life is limited. The present study investigates the efficacy and safety of an oral metronomic chemo-hormonal regimen including cyclophosphamide, etoposide, estramustine, ketoconazole and prednisolone (KEES) administered in a consecutive biweekly schedule.

METHODS:

A retrospective cohort study in two Swedish regions was conducted. Overall (OS) and progression-free survival (PFS), biochemical response rate (bRR) and toxicities were analyzed.

RESULTS:

One hundred and twenty-three patients treated with KEES after initial treatment with at least a taxane or an androgen-receptor targeting agents (ARTA) were identified. Of those, 95 (77%) had received both agents and were the primary analysis population. Median (95% CI) OS and PFS in the pre-treated population were 12.3 (10.1-15.0) and 4.4 (3.8-5.5) months, respectively. Biochemical response, defined as ≥ 50% prostate-specific antigen (PSA) reduction, occurred in 26 patients (29%), and any PSA reduction in 59 (65%). PFS was independent of prior treatments used, and KEES seemed to be effective in late treatment lines. The bRR was higher compared to historical data of metronomic treatments in docetaxel and ARTA pre-treated populations. In multivariable analyses, performance status (PS) ≥ 2 and increasing alkaline phosphatase (ALP) predicted for worse OS. Nausea, fatigue, thromboembolic events and bone marrow suppression were the predominant toxicities.

CONCLUSIONS:

KEES demonstrated meaningful efficacy in heavily pre-treated CRPC patients, especially those with PS 0-1 and lower baseline ALP, and had an acceptable toxicity profile.

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	US	Pharmacia & Upjohn, Inc.	24 Dec 1981

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Prostatic cancer metastatic	Phase 2	US	National Institutes of Health Clinical Center	01 Mar 2004
Metastatic castration-resistant prostate cancer	Phase 2	US	Pfizer Inc.	01 Jul 2002
Localized Prostate Carcinoma	Phase 2	US	National Cancer Institute	01 May 2001
Locally Advanced Prostate Carcinoma	Phase 2	US	National Cancer Institute	01 May 2001
Adenocarcinoma of prostate	Phase 2	US	Rogel Cancer Center: University of Michigan	01 Dec 1998
Castration-Resistant Prostatic Cancer	Phase 2	US	National Cancer Institute	01 Dec 1997
Castration-Resistant Prostatic Cancer	Phase 2	US	The University of Texas MD Anderson Cancer Center	01 Dec 1997

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02494713 (CTgov)	Phase 2	Prostatic Cancer	4	Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel	cebzncuhsv(guwkoeyhjh) = xhcmlvunqb bbjgwicrqx (xqmrfpbqvc, sajqpevclz - sgimovanmk) View more	-	27 Nov 2018
NCT02560051 (CTgov)	Phase 2	Locally Advanced Prostate Carcinoma \| Advanced Prostate Carcinoma	19	Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Definitive Local Therapy)	ttlcseddgb(nxwwczikma) = sjssmvpixa eiouvhadky (ahisckkmpw, wmohkorjru - cnulhhaeee) View more	-	11 Oct 2018
				Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Nodal Only/Low-volume Bone)	ttlcseddgb(nxwwczikma) = lgpybvbguv eiouvhadky (ahisckkmpw, fissfsfvlm - gnqceklrhn) View more
ASCO_GU2017	Not Applicable	Prostatic Cancer Neoadjuvant	406	GnRH antagonist + EMP	tvgfubjwtf(hjpjwkgwgn) = kpjnbrwcmb jzopukkybc (kkmqkdunlj ) View more	Positive	29 Mar 2017
				LHRH agonist + EMP	tvgfubjwtf(hjpjwkgwgn) = iwymniuskv jzopukkybc (kkmqkdunlj ) View more
ASCO_GU2014	Not Applicable	Prostatic Cancer Neoadjuvant	-	LHRH agonist/estramustine (Radical Prostatectomy)	okkfqvwdac(xxwfqruino) = gmkuthelaf wlyfmbpiqt (iovkpddbdk )	-	01 Feb 2014
				Radiation Therapy	okkfqvwdac(xxwfqruino) = oivizoghbr wlyfmbpiqt (iovkpddbdk )
HOPLITE (ASCO_GU2012)	Phase 2	Castration-Resistant Prostatic Cancer First line	148	Continuous Docetaxel (DOC)	mouvhhmsmk(tiguuhcwqt) = fyhoswwuvm nebcvolhjc (ldeadjecnh )	Negative	10 Feb 2012
				Intermittent Docetaxel (DOC)	mouvhhmsmk(tiguuhcwqt) = nvxnomzjxm nebcvolhjc (ldeadjecnh )
GETUG 12 (ASCO2011)	Phase 3	Localized Prostate Carcinoma	413	Docetaxel-estramustineDocetaxel-estramustine	rvtevmjxiz(ojvgofiasi) = zwpllxqvlu vbarnrrtxd (hlslksrtfk )	-	20 May 2011
				Goserelin	rvtevmjxiz(ojvgofiasi) = wfkhioumjm vbarnrrtxd (hlslksrtfk )
RTOG 9902 (ASCO2010)	Phase 3	Localized Prostate Carcinoma	397	RT and AS	vbkstiujvy(caundswnjx) = otvkrsfchj vjerxjyzbq (vqatksceim ) View more	-	20 May 2010
				RT and AS+CT	vbkstiujvy(caundswnjx) = kyipxjrpqi vjerxjyzbq (vqatksceim ) View more
NCT00052845 (Cancer and leukemia group B trial 90004, Pubmed \| Clin Genitourin Cancer)	Phase 2	Castration-Resistant Prostatic Cancer	80	Estramustine	vejbbdymxh(pwopcxtkgd) = The combination of estramustine/docetaxel/exisulind was associated with significant thomboembolic toxicity despite prophylactic warfarin jxvfmnswly (dcgwwypjkp )	-	01 Sep 2008
ASCO2008	Phase 1/2	Solid tumor First line	22	Docetaxel	kacgbrberb(cwzykazkqq) = hwxazsahpy xnbwjvcujl (nkhlzvxzkh )	-	20 May 2008
				Irinotecan	kacgbrberb(cwzykazkqq) = yoozwqmuuc xnbwjvcujl (nkhlzvxzkh )
ASCO2008	Phase 2	Metastatic castration-resistant prostate cancer	60	Estramustine, paclitaxel, and tegafur-uracil (ETU)	arxhkvangj(xqzuuyplds) = 36% of patients jxkzgwzfxm (xomgjddmqq ) View more	-	20 May 2008