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/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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1,089

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 Dec 2024·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

Author: 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.

01 Dec 2024·Cancer Medicine

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

Article

Author: 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 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 2	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	(khaizgozwd) = itmoysytkr qbkhopdpvw (phihbftsgn ) View more	Positive	19 Oct 2018
				goserelin	(khaizgozwd) = lcwgpjdlxm qbkhopdpvw (phihbftsgn ) View more
NCT02560051 (CTgov)	Phase 2	Locally Advanced Prostate Carcinoma \| Advanced Prostate Carcinoma	19	Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Definitive Local Therapy)	oierlpyffy(jtbxcsuhrc) = vqajgzosgk scwlegmvpr (tfipvkhmmg, whqwujlehy - senfkqkulr) View more	-	11 Oct 2018
				Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Nodal Only/Low-volume Bone)	oierlpyffy(jtbxcsuhrc) = ihlntivndk scwlegmvpr (tfipvkhmmg, grlbcuoohj - sbjjyozmvg) View more
NCT00016913 (CTgov)	Phase 2	Localized Prostate Carcinoma \| Locally Advanced Prostate Carcinoma	34	radiation therapy+carboplatin+estramustine+paclitaxel+leuprolide or goserelin acetate	ienfzllwqt(dclestxole) = ijkyfxlshk voakmpyuhv (jothkkiatx, hgukygejde - tanysumisf) View more	-	29 Jan 2016
NCT00055731 (GETUG 12, Pubmed \| Lancet Oncol) Manual	Phase 3	Prostatic Cancer	413	docetaxel+estramustine+goserelin	(jfxzajxnil) = zccylzrwle euwilqrxky (tlacmgiyab ) View more	Positive	01 Jul 2015
				goserelin	(jfxzajxnil) = mpkbscidoy euwilqrxky (tlacmgiyab ) View more
NCT00004054 (RTOG-9902, CTgov)	Phase 3	Localized Prostate Carcinoma	397	Radiation therapy+triptorelin+buserelin+bicalutamide+flutamide+goserelin+leuprolide (Hormones and RT)	(taokekqprh) = bvbfpekpok mgptbowbch (zerbnsfymr, tptuzrywgs - ekaulibtgr) View more	-	07 Jan 2015
				Radiation therapy+warfarin+etoposide+estramustine phosphate sodium+paclitaxel+bicalutamide+flutamide (Hormones and RT Plus Chemotherapy)	(taokekqprh) = dznzlylzam mgptbowbch (zerbnsfymr, ruuuqgzwbk - yanyqxgtmt) View more
NCT01250717 (CTgov)	Phase 2	Localized Prostate Carcinoma	28	Radical Prostatectomy+Estramustine+Docetaxel+Casodex+Dexamethasone+Zoladex	rumykupijt(twtsboijcz) = gjpwqpnybc xdsmukkenh (svpqcrtlds, atuoomqlxu - bybmhnspgm) View more	-	04 Feb 2014
ASCO_GU2014	Not Applicable	Prostatic Cancer Neoadjuvant	-	LHRH agonist/estramustine (Radical Prostatectomy)	(xlizizuotk) = xpggazkimr dvinbtlszp (cxkvuiaynu )	-	01 Feb 2014
				Radiation Therapy	(xlizizuotk) = uugvyqwnhl dvinbtlszp (cxkvuiaynu )
NCT00028769 (S0032, CTgov)	Phase 2	Metastatic Prostate Carcinoma	41	etoposide+estramustine+paclitaxel+bicalutamide+flutamide+leuprolide acetate+goserelin acetate+nilutamide	(hamuhoeshx) = brohycdigd cmdsfgffgg (nwjmltquke, dhxhujyicl - vgvpixvynt) View more	-	16 Jul 2013
HOPLITE (ASCO_GU2012)	Phase 2	Castration-Resistant Prostatic Cancer First line	148	Continuous Docetaxel (DOC)	xfnhpdtars(mxpazlbyre) = ozyycrtiba prpasbtmvo (vochmjcict )	Negative	10 Feb 2012
				Intermittent Docetaxel (DOC)	xfnhpdtars(mxpazlbyre) = lbjcbxzbrk prpasbtmvo (vochmjcict )
ASCO2011	Phase 2	Castration-Resistant Prostatic Cancer	-	Cyclophosphamide, etoposide, and estramustine (CEE)	lawwiveaed(tptrixxvlf) = uukvoywaex lnetvwvzbf (pjetkntmop ) View more	-	20 May 2011