Delving into the Latest Updates on Estramustine Phosphate Sodium with Synapse

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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Literatures (Medical) associated with Estramustine Phosphate Sodium

01 May 2025·The Prostate

Impact of Neoadjuvant Chemohormonal Therapy With GnRH Antagonist and Low‐Dose Estramustine in Very High‐Risk Prostate Cancer Undergoing Robotic Radical Prostatectomy

Article

Author: Kawakita, Mutsushi ; Kambe, Takanari ; Shimatani, Kimihiro ; Negoro, Hiromitsu ; Hattori, Yuto ; Sawada, Atsuro ; Kubota, Masashi ; Kurahashi, Ryoma ; Goto, Takayuki ; Yamasaki, Toshinari ; Kobayashi, Takashi ; Tohi, Yoichiro ; Murata, Shiori ; Saito, Ryoichi ; Sekine, Yuya

ABSTRACTBackgroundHigh‐risk patients with prostate cancer (PC) frequently experience biochemical recurrence (BCR) after surgery. Thus numerous studies have investigated the efficacy of neoadjuvant therapies for high‐risk PC patients; however, no protocol has been established. This study aimed to assess the effect of androgen deprivation therapy combined with low‐dose estramustine phosphate (EMP) on BCR compared with androgen deprivation therapy (ADT) alone in high‐ and very high‐risk patients with PC.MethodsThis retrospective study targeted patients with PC meeting the National Comprehensive Cancer Network high‐risk criteria (cT1‐4N0M0), with 173 patients in the exposure group who received neoadjuvant chemohormonal therapy (gonadotropin‐releasing hormone [GnRH] antagonist combined with low‐dose EMP), and 490 patients in the control group treated with and neoadjuvant hormone therapy (NHT) (ADT ± first‐generation anti‐androgens). Data for each group were extracted from a database of patients who underwent robot‐assisted laparoscopic prostatectomy at 25 tertiary care centers across Japan between 2011 and 2023. The inverse probability of treatment weighting was used to adjust for baseline differences. The primary outcome was BCR‐free survival, with hazard ratios (HRs) calculated using a Cox proportional hazards model between the high‐risk and very high‐risk groups.ResultsAfter adjustment, the standardized mean difference was < 0.1. The exposure group had 3 and 5‐year BCR‐free survival rates of 82.1% and 74.6%, respectively, compared with 70.8% and 64.4% in the control group (HR: 0.55; 95% confidence interval [CI]: 0.35–0.88). For high‐risk patients, the rates were 87.1% and 84.2% at both 3 and 5 years in the intervention group and 83.5% and 75.0% in the control group (HR: 0.66; 95% CI: 0.30–1.47). For very high‐risk patients, the 3‐year and 5‐year rates were 75.3% and 65.7% in the intervention group and 57.3% and 53.6% in the control group (HR: 0.53; 95% CI: 0.30–0.92).ConclusionsIn patients with very high‐risk PC undergoing robot‐assisted laparoscopic prostatectomy, a GnRH antagonist and low‐dose EMP yielded better BCR‐free survival outcomes than NHT.

01 Apr 2025·Journal of Pharmaceutical Sciences

Optimization of HPLC method for determination of Abraham solvation parameters of pharmaceuticals

Article

Author: Knašienė, Birutė ; Sadaunykas, Audrius ; Sazonovas, Andrius ; Balčiūnas, Simonas ; Naujalis, Evaldas ; Lanevskij, Kiril

Abraham solvation equation (Absolv) is a popular and well-established approach for modeling solute partitioning between phases of different polarity, which finds its applications in both organic chemistry and biomedical fields. Parameters constituting this equation are good quantitative descriptors of solute hydrogen bonding potential that are useful for QSAR modeling of more complex chemical and biological phenomena. Numerous studies dealing with fast determination of Abraham descriptors using HPLC can be found in the literature, but these mostly focus on small un-ionizable industrial and environmental chemicals, whereas experimental data for pharmaceutical molecules are clearly lacking. In the current study we build upon a previously published chromatographic approach, aiming to adapt the method to ionizable drug-like compounds, and optimize it by reducing the number of required HPLC columns. The analysis involves determination of the overall H-bond acidity (A), H-bond basicity (B) and polarity/polarizability (S) descriptors for 62 pharmaceutical molecules with previously unpublished parameter values.

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.

100 Deals associated with Estramustine Phosphate Sodium

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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	Japan	Nippon Shinyaku Co., Ltd.	22 Mar 2007

Developing

10 top R&D records.

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

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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	(aragsaauhl) = ldwpskeags fwgnkauuob (fxpkzhwzta ) View more	Positive	19 Oct 2018
				goserelin	(aragsaauhl) = dsqtfnevtm fwgnkauuob (fxpkzhwzta ) View more
NCT02560051 (CTgov)	Phase 2	Locally Advanced Prostate Carcinoma \| Advanced Prostate Carcinoma	19	Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Definitive Local Therapy)	tnokyhgmfe(uqsssrczvi) = akdeuhxfiw pdpmluvlep (krfapwdthc, gaiplcawmo - vqzqzpvoyq) View more	-	11 Oct 2018
				Estramustine+Doxorubicin+Degarelix+Ketoconazole+Docetaxel (Nodal Only/Low-volume Bone)	tnokyhgmfe(uqsssrczvi) = oaufbkqbuv pdpmluvlep (krfapwdthc, lgbtznouug - ghdqtnxsmk) View more
NCT00016913 (CTgov)	Phase 2	Localized Prostate Carcinoma \| Locally Advanced Prostate Carcinoma	34	radiation therapy+carboplatin+estramustine+paclitaxel+leuprolide or goserelin acetate	pmwmtupypy(xpnwblvuwf) = spztltjrsw xzbxeujjkh (qrfhqfslua, sufiizsaua - icjoqusdrs) View more	-	29 Jan 2016
NCT00055731 (GETUG 12, Pubmed \| Lancet Oncol) Manual	Phase 3	Prostatic Cancer	413	docetaxel+estramustine+goserelin	(gjjldarpkx) = vwefeglzxy udvkkyvjmo (sstqbvoupl ) View more	Positive	01 Jul 2015
				goserelin	(gjjldarpkx) = rfpubfmdam udvkkyvjmo (sstqbvoupl ) View more
NCT00004054 (RTOG-9902, CTgov)	Phase 3	Localized Prostate Carcinoma	397	Radiation therapy+triptorelin+buserelin+bicalutamide+flutamide+goserelin+leuprolide (Hormones and RT)	(ifkglvbkny) = ocdopfools pdhxgikpwl (yjlafaiavw, fvhnjdxhsc - qfwhquyoqv) View more	-	07 Jan 2015
				Radiation therapy+warfarin+etoposide+estramustine phosphate sodium+paclitaxel+bicalutamide+flutamide (Hormones and RT Plus Chemotherapy)	(ifkglvbkny) = pbiphldjgy pdhxgikpwl (yjlafaiavw, zuahawunek - heptkpcfvs) View more
NCT01250717 (CTgov)	Phase 2	Localized Prostate Carcinoma	28	Radical Prostatectomy+Estramustine+Docetaxel+Casodex+Dexamethasone+Zoladex	vegykliinv(njgwlehivt) = fxjxualbjk tmdrzkavob (eildinmnat, rindbpxvbt - rtruzkvkic) View more	-	04 Feb 2014
ASCO_GU2014	Not Applicable	Prostatic Cancer Neoadjuvant	-	LHRH agonist/estramustine (Radical Prostatectomy)	(neyatclwyg) = xyargvkysx rewlkrrvom (olsfprqmvo )	-	01 Feb 2014
				Radiation Therapy	(neyatclwyg) = dhjlbqmfsv rewlkrrvom (olsfprqmvo )
NCT00028769 (S0032, CTgov)	Phase 2	Metastatic Prostate Carcinoma	41	etoposide+estramustine+paclitaxel+bicalutamide+flutamide+leuprolide acetate+goserelin acetate+nilutamide	(lswshuhylr) = ygrpuzaysn wjzqfxbifa (bcpazurcim, ochgmxvyen - wrlwbepvzp) View more	-	16 Jul 2013
HOPLITE (ASCO_GU2012)	Phase 2	Castration-Resistant Prostatic Cancer First line	148	Continuous Docetaxel (DOC)	zszcdryxep(ovdozymocq) = bewgnlqmck yowawklcgi (sbdjglmyjl )	Negative	10 Feb 2012
				Intermittent Docetaxel (DOC)	zszcdryxep(ovdozymocq) = zfxpkgawhu yowawklcgi (sbdjglmyjl )
ASCO2011	Phase 2	Castration-Resistant Prostatic Cancer	-	Cyclophosphamide, etoposide, and estramustine (CEE)	hqqxjdhtkt(acwzturyyc) = itfpyzvegd pjwxtiektg (gzdhwqvduk ) View more	-	20 May 2011