雌二醇屈螺酮(Drospirenone/Estradiol) - 药物靶点：AR x ER x MR x PR_在研适应症：更年期综合症，绝经期后骨质疏松，血管疾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Angeliq、Angeliq low-low、Estradiol and Drospirenone

+ [8]

靶点

AR x ER x MR x PR

作用机制

AR拮抗剂(雄激素受体拮抗剂)、ERs激动剂(雌激素受体家族激动剂)、MR拮抗剂(盐皮质激素受体拮抗剂)

治疗领域

心血管疾病内分泌与代谢疾病皮肤和肌肉骨骼疾病+ [2]

在研适应症

更年期综合症绝经期后骨质疏松血管疾病+ [3]

非在研适应症

原发性高血压高血压高血压前期

原研机构

Bayer AG

在研机构

Searchlight Pharma, Inc.初创企业

Bayer HealthCare Pharmaceuticals, Inc.Bayer Vital GmbH

非在研机构

Bayer AG

最高研发阶段批准上市

首次获批日期

美国 (2005-09-28),

血管舒缩症外阴和阴道萎缩

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C42H54O5

InChIKeyQJUXBIVLOGRZSQ-OQMMLGNJSA-N

CAS号350818-73-4

关联

12

项与雌二醇屈螺酮相关的临床试验

NCT03126773

/ CompletedN/A

A Prospective Multicenter Non-interventional Cohort Study on Patients'Satisfaction With Angeliq® Micro in Real Clinical Practice Conducted in Russia

To evaluate the patients' satisfaction with Angeliq Micro in real clinical practice after 13 cycles of treatment.

开始日期2017-05-02

申办/合作机构

Bayer AG

NCT01109979

/ Completed临床4期IIT

Effect of Combined Estradiol and Drospirenone Treatment Versus Combined Estradiol and Medroxyprogesterone Acetate Treatment on Endothelial Function: A Crossover Study

This study compares the effects of two common hormone medications on the heart and blood vessels of healthy post-menopausal women over the age of 45.
The study will take place over the course of about 5 months. Each subject will take two different medications over two six-week periods. They will be randomized at the beginning of the study to either estradiol+medroxyprogesterone acetate or estradiol+drospirenone for the first period, and will receive the other medication the second six-weeks of the study. At the very beginning of the study and at the end of each six-week treatment period, subjects will come to the hospital various tests including non-invasive blood vessel imaging tests, blood draws to test the levels of certain hormones in the body, an oral glucose tolerance test, a test to monitor renal blood flow, and 24-hour blood pressure monitoring. Between treatment periods, there will be a four-week medication-free washout period.

开始日期2009-12-01

申办/合作机构

The Brigham & Women's Hospital, Inc.

[+1]

NCT00785317

/ Unknown status临床4期

Effects of Oral 1 mg Oestradiol (E2)/ 2 mg of Drospirenone (DRSP) Compared to Oral 1 mg of Oestradiol (E2)/ 0.5 mg Noresthisterone Acetate (NETA)on the Postmenopausal Breast; a Double Blind Randomized Prospective Study

The purpose of this study is to evaluate the effects on breast in postmenopausal women randomized to either oestradiol in combination with DRSP or E2 in combination with NETA during six months.

开始日期2008-11-01

申办/合作机构

Karolinska Institutet

100 项与雌二醇屈螺酮相关的临床结果

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100 项与雌二醇屈螺酮相关的转化医学

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100 项与雌二醇屈螺酮相关的专利（医药）

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29

项与雌二醇屈螺酮相关的文献（医药）

2018-01-01·Kardiologiia4区 · 医学

Structural and functional changes of blood vessels in women in early postmenopause, the possibility of correction of the revealed violations

4区 · 医学

Article

作者: Rebrov, A P ; Salov, I A ; Tolstov, S N

AIM:

To evaluate severity and pattern of structural and functional changes of vascular wall in early postmenopausal women receiving chronic treatment with a low-dose combination of 17β-estradiol (E2) 1 mg and drospirenone 2 mg (DRSP). Evaluation of structural and functional arterial remodeling might be important for assessment of cardiovascular risk in postmenopausal women.

MATERIALS AND METHODS:

The study included 162 early postmenopausal women with postmenopausal syndrome. The women were divided into two groups. The main group consisted of 84 patients receiving the postmenopausal hormonal therapy (PMHT) with E2 1 mg / DRSP 2 mg (Angeliq, Bayer) and the control group included 78 women not receiving PMHT. The follow-up duration was 5.2 years. 24‑h blood pressure monitoring with evaluation of arterial stiffness (RWTT, AIx, ASI, AASI, (dP/dt) max) was performed. Endothelium-dependent dilation of the brachial artery was measured using the reactive hyperemia test. Aortic pulse wave velocity (aPWV) and common carotid intima-media thickness (ccIMT) were measured ultrasonically.

RESULTS:

At baseline, increased aPWV was observed in 15 (21.4 %) women of the main group and 19 (24.3 %) women of the control group (р=0.4). At the end of study, increased aPWV was observed in both groups but the increase was more pronounced in the control group. Increased pulse blood pressure (PBP) was observed in 27 (32.1 %) patients of the main group and 26 (33.3 %) patients of the control group (р=0.87). At the end of study, PBP decreased from 47.2±7.2 to 45.3±6.9 mm Hg (р.

2015-06-16·Zhonghua yi xue za zhi

[Clinical and metabolic effects of drospirenone-estradiol versus tibolone in postmenopausal women:a comparative study].

Article

作者: Cheng, Jiao ; Zhang, Zhenyu

OBJECTIVE:

To compare the clinical and metabolic effects of drospirenone-estradiol (Angeliq) versus tibolone (Livial) in postmenopausal women.

METHODS:

Twenty-seven postmenopausal women of group 1 took Angeliq (1 dose every two days) while another group 2 (n = 26) received tibolone (2.5 mg every two days) as hormone replacement therapy for 12 weeks. A retrospective analysis was used to evaluate the clinical efficacy, safety and risk factors of cardiovascular metabolism. The clinical data were collected before and after treatment, including personal interview, medical examination and ultrasound imaging of pelvic, breast and carotid artery.

RESULTS:

No statistically significant inter-group differences existed in age or body mass index. Before treatment, the level of E2 was (12 ± 10) ng/L, triglyceride (TG) (2.0 ± 1.1) mmol/L, lipoprotein-a (LPa) (47 ± 43) mmol/L in group 1 versus (23 ± 12) ng/L, (1.3 ± 0.7) mmol/L and (28 ± 14) mmol/L in group 2. After 12-week treatment, (30 ± 18) ng/L, (1.6 ± 1.1) mmol/L and (37 ± 36) mmol/L in group 1 versus (23 ± 9) ng/L, (1.1 ± 0.6) mmol/L and (18 ± 12) mmol/L in group 2. A greater incidence of vaginal bleeding and thicker endometrium were found in group 1.

CONCLUSION:

Angeliq can relieve menopausal symptoms. And its functions of regulating lipid metabolism and protecting cardiovascular system are better than those of Livial. However, its wider acceptability is limited by vaginal bleeding, thicker endometrium and breast pain.

2014-07-01·Maturitas3区 · 医学

Treatment of climacteric symptoms in breast cancer patients: A retrospective study from a medication databank

3区 · 医学

Article

作者: Rozenberg, Serge ; Paesmans, Marianne ; Ameye, Lieveke ; Antoine, Caroline

INTRODUCTION:

Women affected by breast cancer (BC) will often go through menopause at an earlier age and display more frequent and severe symptoms than women who have a natural menopause. The safety of hormone replacement therapy (HRT) and vaginal estrogens for BC survivors has been debated over time and remains unclear. Non hormonal therapies such as antidepressants, gabapentine and clonidine may be useful for those patients but there are few data about their safety.

AIM:

This retrospective study analyses the use by BC patients of treatments known to alleviate climacteric symptoms.

MATERIAL AND METHOD:

Post-menopausal Estrogen Receptors positive (ER+) BC patients, aged 45-69, were identified as having bought, at least once, an aromatase inhibitor (AI) or tamoxifen between the years 2000 and 2012 through a pharmaceutical databank in Belgium. Among them, we defined users of a climacteric treatment those who bought, at least once, HRT, vaginal topical estrogens, antidepressants, clonidine and gabapentine.

RESULTS:

We identified 2530 BC patients. Among them, 45% were buying a treatment known to alleviate menopausal symptoms. The majority of these treatments were non-HRT therapies. HRT and vaginal estrogens were seldom bought (respectively 1.1% and 6%), but 3% bought vaginal estrogens while buying AI. About 9.2% of tamoxifen users patients bought antidepressants implicated in tamoxifen metabolism at the same time as tamoxifen.

CONCLUSIONS:

Most BC patients follow current guidelines contra-indicating the use of HRT after BC, they use non hormonal therapies. In some cases they use unfortunately antidepressants that may alter the metabolism of tamoxifen.

100 项与雌二醇屈螺酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	雌二醇屈螺酮	G03AA G03FA	-

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
更年期综合症	中国	Bayer HealthCare Pharmaceuticals, Inc.	2015-01-11
绝经期后骨质疏松	中国	Bayer Vital GmbH	2009-09-29
血管疾病	中国	Bayer Vital GmbH	2009-09-29
血管舒缩症	美国	Bayer HealthCare Pharmaceuticals, Inc.	2005-09-28
外阴和阴道萎缩	美国	Bayer HealthCare Pharmaceuticals, Inc.	2005-09-28
避孕	加拿大	Searchlight Pharma, Inc.初创企业	-

未上市

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适应症	最高研发状态	国家/地区	公司	日期
原发性高血压	临床3期	-	Bayer AG	2004-04-01
高血压	临床2期	美国	Bayer AG	2007-01-01
高血压前期	临床2期	美国	Bayer AG	2007-01-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01109979 (CTgov)	临床4期	心血管疾病	24	Estradiol (E)+medroxyprogesterone acetate (MPA) (E+MPA)	遞膚窪顧廠簾夢壓窪壓(築鹽艱醖醖襯簾憲鬱築) = 獵鹽願觸鑰壓鬱簾窪夢膚艱遞窪膚壓鏇範範餘 (範願窪衊觸範襯鹹遞鹽, 鏇醖鹽醖顧夢糧鏇鹹夢 ~ 獵襯顧餘壓憲憲艱夢窪) 更多	-	2013-05-03
				Drospirenone (DRSP) (E+DRSP)	遞膚窪顧廠簾夢壓窪壓(築鹽艱醖醖襯簾憲鬱築) = 鏇簾艱襯淵蓋窪壓願繭膚艱遞窪膚壓鏇範範餘 (範願窪衊觸範襯鹹遞鹽, 衊簾顧觸餘願鏇艱夢糧 ~ 憲顧範顧艱鹹廠壓鏇膚) 更多
NCT00522873 (CTgov)	临床3期	-	662	0.25mg DRSP / 0.5mg E2 (BAY86-4891) (0.25mg DRSP / 0.5mg E2 (BAY86-4891))	築憲憲選醖糧簾夢蓋簾(觸簾遞壓淵廠積積衊網) = 選顧鹽顧築獵構鹹簾鹽獵壓壓網築餘鹽艱艱鏇 (窪鹹積獵窪網積網網醖, 夢衊範艱網糧襯獵鑰艱 ~ 壓憲簾簾糧衊積蓋齋鬱) 更多	-	2012-06-28
				0.5mg NETA / 1.0mg E2 (Activella) (0.5mg NETA / 1.0mg E2 (Activella))	襯蓋鹹願齋鏇餘鏇鹽醖(觸獵積餘壓範鬱鹹鬱獵) = 遞繭淵鹽願醖簾鑰齋製構襯衊構醖壓醖蓋衊願 (築憲醖遞膚簾艱願製網, 製蓋鹽鹽網顧範壓鹹範 ~ 襯顧餘願遞壓壓憲願鏇) 更多
NCT00420342 (CTgov)	临床2期	高血压 \| 高血压前期	92	Drospirenone/17ß-estradiol (Angeliq, BAY86-4891) (0.5mg DRSP / 1.0mg E2 (Angeliq, BAY86-4891))	鑰淵構衊廠憲觸艱衊餘(鑰選簾衊襯積壓襯觸憲) = 觸壓繭膚築觸鹹艱網廠繭積顧鬱積壓積糧築製 (鑰淵顧蓋網願鏇糧夢鑰, 簾醖願憲鹹淵窪蓋餘襯 ~ 顧膚糧淵網觸廠獵製淵) 更多	-	2010-01-20
				Drospirenone/17ß-estradiol (Angeliq, BAY86-4891) (2.0mg DRSP / 1.0mg E2 (Angeliq, BAY86-4891))	鑰淵構衊廠憲觸艱衊餘(鑰選簾衊襯積壓襯觸憲) = 鹽築獵鑰淵糧構網製鬱繭積顧鬱積壓積糧築製 (鑰淵顧蓋網願鏇糧夢鑰, 窪網艱衊構範鏇糧膚構 ~ 醖網窪糧構窪鬱憲膚蓋) 更多