Delving into the Latest Updates on Estradiol-3-O-sulfamate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Estradiol 3-sulfamate

+ [3]

Target

ER x STS

Action

agonists, inhibitors

Mechanism

ERs agonists(Estrogen receptors agonists), STS inhibitors(Steryl-sulfatase inhibitors)

Therapeutic Areas

Urogenital DiseasesEndocrinology and Metabolic Disease

Active Indication-

Inactive Indication

EndometriosisOestrogen deficiency

Originator Organization

Jenapharm GmbH & Co. KG

Active Organization-

Inactive Organization

PregLem SABayer Schering Pharma AG

License Organization-

Drug Highest PhasePendingPhase 2

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC18H25NO4S

InChIKeyYXYXCSOJKUAPJI-ZBRFXRBCSA-N

CAS Registry172377-52-5

This is a Phase II, multicentre, randomised, two-arm, parallel group ,double-blind, placebo controlled, study to investigate the efficacy, safety, pharmacokinetics and pharmacodynamics of the steroid sulfatase inhibitor PGL2001 with concomitant, continuous NETA administration for the treatment of pain symptoms suggestive of endometriosis. The target population will be women of reproductive age with symptoms suggestive of endometriosis.

Start Date01 Jun 2012

Sponsor / Collaborator

PregLem SA

EUCTR2011-005167-24-HU

/ Not yet recruitingPhase 2

A Phase II, Multicentre, Randomised, Two-Arm, Parallel Group, Double-Blind, Placebo controlled Study of the Steroid Sulfatase Inhibitor PGL2001 with concomitant administration of NETA (norethisterone acetate) for the treatment of symptoms related to endometriosis - AMBER

Start Date04 May 2012

Sponsor / Collaborator-

100 Clinical Results associated with Estradiol-3-O-sulfamate

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100 Translational Medicine associated with Estradiol-3-O-sulfamate

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100 Patents (Medical) associated with Estradiol-3-O-sulfamate

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35

Literatures (Medical) associated with Estradiol-3-O-sulfamate

01 Mar 2025·Industrial Crops and Products

Beneficial microbial consortia effectively alleviated plant stress caused by the synergistic toxicity of microplastics and cadmium

Author: Gao, Shan-Shan ; Li, Yu-Ying ; Zhang, Yu ; Li, B. Larry ; Han, Hui ; Chen, Zhao-Jin ; Chen, Yan ; Jiao, Rui-Qi

Combined pollution from microplastics and heavy metals has garnered research interest because of the potential for complex interactions between these contaminants.Composite functional bacteria present significant benefits in the bioremediation of contaminated soils and have attracted widespread attention.Researchers have yet to elucidate how effectively plant growth-promoting bacterial (PGPB) consortia mitigate the stress induced by combined pollution from microplastics and heavy metals.Pot experiments indicate that combined polyvinyl chloride (PVC) + cadmium (Cd) pollution results in "synergistic toxicity" relative to Cd or PVC pollution alone.The application of PGPB consortia inoculants is more effective than the use of single strains in alleviating stress caused by PVC + Cd pollution.The combined inoculant increased bioenergy plant sorghum growth and biomass and increased the contents of total nitrogen, total phosphorus, total potassium, available potassium, and available phosphorus in the soil.Under combined PVC + Cd pollution conditions, PGPB inoculation affected the composition of the sorghum rhizosphere bacterial community.Cooccurrence network anal. revealed that the PGPB consortia can alter soil bacterial community diversity and increase the stability of soil bacterial communities.PGPB consortia can alter the composition of soil metabolites and impact various metabolic pathways.These changes increase the ability of sorghum plants to respond to PVC + Cd stress.This study revealed that the use of combined PGPB affects the soil inorganic nutrient content and the functional composition of bacterial communities, effectively alleviating stress caused by combined microplastic and heavy metal pollution.These findings provide tech. support for the development of bioremediation strategies tailored to address combined microplastic and heavy metal pollution.

05 Aug 2020·ChemMedChemQ3 · MEDICINE

Synthesis of Tamoxifen‐Artemisinin and Estrogen‐Artemisinin Hybrids Highly Potent Against Breast and Prostate Cancer

Q3 · MEDICINE

Article

Author: Morozkina, Svetlana N. ; Tsogoeva, Svetlana B. ; Fröhlich, Tony ; Friedrich, Oliver ; Gilbert, Daniel F. ; Shavva, Alexander G. ; Mai, Christina ; Bogautdinov, Roman P.

AbstractIn the search for new and effective treatments of breast and prostate cancer, a series of hybrid compounds based on tamoxifen, estrogens, and artemisinin were successfully synthesized and analyzed for their in vitro activities against human prostate (PC‐3) and breast cancer (MCF‐7) cell lines. Most of the hybrid compounds exhibit a strong anticancer activity against both cancer cell lines – for example, EC50 (PC‐3) down to 1.07 μM, and EC50 (MCF‐7) down to 2.08 μM – thus showing higher activities than their parent compounds 4‐hydroxytamoxifen (afimoxifene, 7; EC50=75.1 (PC‐3) and 19.3 μM (MCF‐7)), dihydroartemisinin (2; EC50=263.6 (PC‐3) and 49.3 μM (MCF‐7)), and artesunic acid (3; EC50=195.1 (PC‐3) and 32.0 μM (MCF‐7)). The most potent compounds were the estrogen‐artemisinin hybrids 27 and 28 (EC50=1.18 and 1.07 μM, respectively) against prostate cancer, and hybrid 23 (EC50=2.08 μM) against breast cancer. These findings demonstrate the high potential of hybridization of artemisinin and estrogens to further improve their anticancer activities and to produce synergistic effects between linked pharmacophores.

01 Oct 2014·Reproductive SciencesQ3 · MEDICINE

Synergistic Effects of E2MATE and Norethindrone Acetate on Steroid Sulfatase Inhibition: A Randomized Phase I Proof-of-Principle Clinical Study in Women of Reproductive Age

Q3 · MEDICINE

Article

Author: Bestel, Elke ; Gotteland, Jean-Pierre ; Pohl, Oliver

The combination of a progestin such as norethindrone acetate (NETA) reducing the ovarian estrogen production with a steroid sulfatase (STS) inhibitor (STS-I) decreasing the local estrogen production could result in a new treatment option for endometriosis. The study reported was a randomized, double-blind, and placebo-controlled study to investigate the pharmacodynamics, pharmacokinetics, and safety of the STS-I PGL2001 (E2MATE) and NETA. A total of 24 healthy women of reproductive age were treated with weekly doses of PGL2001 or daily doses of NETA or a combination of both compounds for 4 weeks. Four weeks of treatment with PGL2001 or PGL2001 + NETA reduced the STS activity in the endometrium by 91% (±3%) and 96% (±4%), respectively, and comparable values were observed 1 month after the treatment was stopped. The combined treatment of PGL2001 + NETA led to significantly higher STS inhibition at both times (P < .01 and P < .05, respectively). This study showed that administration of PGL2001 alone at 4 mg/week or combined with NETA to healthy women of reproductive age led to STS inhibition and changes in functional STS biomarkers in the endometrium, resulting in synergistic effects of PGL2001 and NETA on STS activity.

100 Deals associated with Estradiol-3-O-sulfamate

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Endometriosis	Phase 2	Hungary	PregLem SA	01 Jun 2012
Endometriosis	Phase 2	Romania	PregLem SA	01 Jun 2012
Endometriosis	Phase 2	Poland	PregLem SA	01 Jun 2012
Oestrogen deficiency	Phase 2	United States	Bayer Schering Pharma AG	01 Jul 2001