Estradiol-3-O-sulfamate(Estradiol-3-O-sulfamate) - 药物靶点：ER x STS_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Estradiol 3-sulfamate

+ [3]

靶点

ER x STS

作用机制

ERs激动剂(雌激素受体家族激动剂)、STS抑制剂(固醇硫酸酯酶抑制剂)

治疗领域

泌尿生殖系统疾病内分泌与代谢疾病

在研适应症-

非在研适应症

子宫内膜异位症雌激素缺乏症状

原研机构

Jenapharm GmbH & Co. KG

在研机构-

非在研机构

PregLem SABayer Schering Pharma AG

最高研发阶段无进展临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C18H25NO4S

InChIKeyYXYXCSOJKUAPJI-ZBRFXRBCSA-N

CAS号172377-52-5

关联

2

项与 Estradiol-3-O-sulfamate 相关的临床试验

NCT01631981 / Completed临床2期

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

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.

开始日期2012-06-01

申办/合作机构

PregLem SA

EUCTR2011-005167-24-HU / Not yet recruiting临床2期

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

开始日期2012-05-04

申办/合作机构-

100 项与 Estradiol-3-O-sulfamate 相关的临床结果

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100 项与 Estradiol-3-O-sulfamate 相关的转化医学

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100 项与 Estradiol-3-O-sulfamate 相关的专利（医药）

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40

项与 Estradiol-3-O-sulfamate 相关的文献（医药）

2023-11-01·Journal of Environmental Management

Assimilation behaviors and metabolite formations of estrone sulfate sodium (E1-3S) and 17β-estradiol-3-O-sulfate sodium (E2-3S) in the wheat

Article

作者: Zhao, Yan ; Shi, Wenzhuo ; Li, Jing ; Li, Yanxia ; Zhang, Xuelian ; Jiang, Linshu ; Jiang, Xiaoman ; Zhang, Shengwei

The conjugated steroid estrogens (CSEs), including estrone sulfate sodium (E1-3 S) and 17β-estradiol-3-O-sulfate sodium (E2-3 S), exhibit distinct metabolic behaviors in the aqueous and soil environments. However, their assimilation behaviors and metabolite formations in plant bodies (shoots and roots) remain poorly understood. Therefore, this study used a modified plant hydroponic system to explore the efficiency with which wheat (Triticum acstivnm L.) assimilated the two estrogen conjugates, E1-3 S and E2-3 S. Results indicated the potential of wheat to absorb E1-3 S and E2-3 S, with their assimilation in the root being significantly higher (10⁴-10⁵ ng/g dw) than in the shoot (10³-10⁴ ng/g dw). E1-3 S de-sulfated and transformed to estrone (E1) at a rate of 4%-45% in the root's oxidative environment, whereas E2-3 S converted to E1-3 S at 210%-570%. However, the root-to-shoot transfer was impeded by a less potent metabolic activity within the shoot system. The co-exposure treatment revealed that E1 or 17β-estradiol (E2) affects the assimilation of E1-3 S and E2-3 S by wheat, with E1 inhibiting E1-3 S assimilation and E2 promoting E2-3 S assimilation in wheat bodies. Nonetheless, free-form steroid estrogens (FSEs), which typically have a significant hormone action, can oxidative-damage the wheat tissues, producing a progressive wilting of wheat leaf and so limiting the transpiration process. Co-exposure initially increased the assimilation amounts of E1-3 S (particularly in shoots) and E2-3 S (in both roots and shoots), but these values rapidly declined as exposure duration increased. The combined effects of E1-3 S and E2-3 S exposure also increased their assimilation. These findings suggest the need for further investigation into the cumulative impact of environmental estrogen contaminants. The findings of present study can potentially guide the development of strategies to prevent and manage steroid estrogen contamination in agricultural contexts.

2014-10-01·Reproductive Sciences3区 · 医学

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

3区 · 医学

Article

作者: 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.

2013-01-01·Expert Opinion on Therapeutic Patents2区 · 医学

Sulfatase inhibitors: a patent review

2区 · 医学

Review

作者: Williams, Spencer J

INTRODUCTIONSteroid sulfatase (STS) converts sulfated hormones to free hormones of importance in hormone-dependent diseases such as breast cancer and endometriosis. Carbohydrate sulfatases degrade complex carbohydrates as part of normal cellular turnover; certain lysosomal storage disorders (LSDs) involve defective processing of sulfated glycosaminoglycans by mutant sulfatases.AREAS COVEREDAryl sulfamates have been developed as STS inhibitors, and STX64 and PGL2001 are under evaluation in Phase I and II clinical trials for treatment of endometrial and metastatic breast and prostate cancers and endometriosis. Dual-acting compounds have emerged that are aromatase inhibitors (AIs), selective estrogen receptor antagonists, or inhibitors of microtubule polymerization. Sulfamidase inhibitors as pharmacological chaperones to assist maturation of folding-defective mutants for the treatment of Sanfilippo type A disease are under investigation. Coverage: The patent literature after the mid-1990s.EXPERT OPINIONThe failure of STX64 in a Phase II monotherapy clinical trial should not dissuade further investigations in multidrug regimens, particularly in combination with AIs. The recent development of dual-acting compounds may enhance the potential for success in the clinic. Further investigations into aryl sulfamates are required to clarify the molecular mechanism of action; additionally, new reversible sulfatase inhibition concepts are needed for the development of pharmacological chaperones for sulfatase LSDs.

100 项与 Estradiol-3-O-sulfamate 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB06597

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
子宫内膜异位症	临床3期	罗马尼亚	PregLem SA	2012-06-01
子宫内膜异位症	临床3期	波兰	PregLem SA	2012-06-01
子宫内膜异位症	临床3期	匈牙利	PregLem SA	2012-06-01
雌激素缺乏症状	临床3期	美国	Bayer Schering Pharma AG	2001-07-01