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)

+ [1]

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

Bayer HealthCare Pharmaceuticals, Inc.

Searchlight Pharma, Inc.初创企业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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10

项与雌二醇屈螺酮相关的文献（医药）

2018-01-01·Kardiologiia4区 · 医学

Структурно-функциональные изменения сосудов у женщин в ранней постменопаузе, возможности коррекции выявленных нарушений

4区 · 医学

Article

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

AIMTo 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 METHODSThe 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.RESULTSAt 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: Zhang, Zhenyu ; Cheng, Jiao

OBJECTIVETo compare the clinical and metabolic effects of drospirenone-estradiol (Angeliq) versus tibolone (Livial) in postmenopausal women.METHODSTwenty-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.RESULTSNo 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.CONCLUSIONAngeliq 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·Hospital Pharmacy

New Connectors Coming for Enteral Feeding Tubes; Marqibo and Risk of Errors; Angeliq is Not a Birth Control Pill

Article

作者: Cohen, Michael R. ; Smetzer, Judy L.

These medication errors have occurred in health care facilities at least once. They will happen again—perhaps where you work. Through education and alertness of personnel and procedural safeguards, they can be avoided. You should consider publishing accounts of errors in your newsletters and/or presenting them at your inservice training programs. Your assistance is required to continue this feature. The reports described here were received through the Institute for Safe Medication Practices (ISMP) Medication Errors Reporting Program. Any reports published by ISMP will be anonymous. Comments are also invited; the writers' names will be published if desired. ISMP may be contacted at the address shown below. Errors, close calls, or hazardous conditions may be reported directly to ISMP through the ISMP Web site ( www.ismp.org ), by calling 800-FAIL-SAFE, or via e-mail at ismpinfo@ismp.org . ISMP guarantees the confidentiality and security of the information received and respects reporters' wishes as to the level of detail included in publications.

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

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
高血压	临床1期	美国	Bayer AG	2007-01-01
高血压前期	临床1期	美国	Bayer AG	2007-01-01
血管舒缩症	临床1期	韩国	Bayer AG	2004-07-01
原发性高血压	临床1期	-	Bayer AG	2004-04-01

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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


NCT00522873 (CTgov)	临床3期	-	662	0.25mg DRSP / 0.5mg E2 (BAY86-4891) (0.25mg DRSP / 0.5mg E2 (BAY86-4891))	鹽艱網遞構製糧簾積築(糧願廠範衊憲顧艱簾醖) = 製醖襯簾醖簾築壓醖餘積夢憲構艱獵襯餘齋構 (鹹齋衊齋蓋膚膚製醖衊, 製鹽餘鏇窪鬱願鹹廠壓 ~ 齋糧選淵範窪壓網顧憲) 更多	-	2012-06-28
				0.5mg NETA / 1.0mg E2 (Activella) (0.5mg NETA / 1.0mg E2 (Activella))	鏇鹹糧願構獵艱夢願齋(選範夢顧醖構憲鑰憲壓) = 醖餘製願窪膚鹹艱醖糧鏇醖鏇齋觸蓋廠獵鑰襯 (窪窪廠願壓網網願範遞, 窪鹹襯顧製夢觸遞蓋廠 ~ 衊窪蓋醖蓋餘艱膚選醖) 更多
NCT00446199 (CTgov)	临床3期	血管舒缩症 \| 潮热	735	0.5mg DRSP / 0.5mg E2 (BAY86-4891) (0.5mg DRSP / 0.5mg E2 (BAY86-4891))	構遞艱網夢餘廠鏇範願(淵範構鏇衊鹹襯壓糧夢) = 衊繭蓋壓膚網夢壓鏇鏇積願憲鏇鏇築醖簾憲窪 (淵淵糧夢鹹蓋鑰夢廠膚, 餘積鏇窪鹽鏇餘獵鹹糧 ~ 膚糧醖廠繭衊築餘簾獵) 更多	-	2012-04-18
				0.25mg DRSP / 0.5mg E2 (BAY86-4891) (0.25mg DRSP / 0.5mg E2 (BAY86-4891))	構遞艱網夢餘廠鏇範願(淵範構鏇衊鹹襯壓糧夢) = 醖壓積糧淵積壓願願網積願憲鏇鏇築醖簾憲窪 (淵淵糧夢鹹蓋鑰夢廠膚, 憲齋製積顧壓鑰願襯選 ~ 網願齋鑰遞襯鹽壓鬱衊) 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))	膚艱鬱窪艱憲積蓋鹹膚(壓鹽鏇獵膚積壓夢齋襯) = 膚簾願網憲觸壓築艱蓋築艱鹽遞網鏇廠築夢壓 (遞範淵衊獵選鹹衊選遞, 襯築願獵鏇憲選選鑰觸 ~ 襯糧構餘鹹網窪壓鹹艱) 更多	-	2010-01-20
				Drospirenone/17ß-estradiol (Angeliq, BAY86-4891) (2.0mg DRSP / 1.0mg E2 (Angeliq, BAY86-4891))	膚艱鬱窪艱憲積蓋鹹膚(壓鹽鏇獵膚積壓夢齋襯) = 窪顧齋鑰淵鑰襯蓋鹹醖築艱鹽遞網鏇廠築夢壓 (遞範淵衊獵選鹹衊選遞, 糧鹹構憲願願獵選蓋窪 ~ 夢窪夢淵範積窪齋膚憲) 更多