地诺孕素/戊酸雌二醇(Dienogest/Estradiol Valerate) - 药物靶点：ER x PR_在研适应症：月经过多，避孕，雌激素缺乏症状_专利_临床

概要

基本信息

药物类型

小分子化药

别名

ESTRADIOL VALERATE/ESTRADIOL VALERATE/DIENOGEST

+ [4]

靶点

ER x PR

作用方式

激动剂

作用机制

ERs激动剂(雌激素受体家族激动剂)、PR激动剂(孕激素受体激动剂)

治疗领域

内分泌与代谢疾病泌尿生殖系统疾病其他疾病+ [1]

在研适应症

非在研适应症

原研机构

在研机构

Bayer HealthCare Pharmaceuticals, Inc.

+ [2]

非在研机构

Bayer AG

最高研发阶段批准上市

首次获批日期

荷兰 (2001-05-08),

雌激素缺乏症状

最高研发阶段(中国)无进展

特殊审评-

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结构/序列

分子式C43H57NO5

InChIKeyLRHSUZNWLAJWRT-GAJBHWORSA-N

CAS号307334-58-3

关联

26

项与地诺孕素/戊酸雌二醇相关的临床试验

TCTR20240908003

/ Not yet recruiting临床4期IIT

A comparison of menstrual volume and other benefits between Estradiol valerate/dienogest and Ethinyl estradiol/desogestrel: A randomized controlled trial

开始日期2024-09-01

申办/合作机构

Srinakharinwirot University

NCT06396208

/ RecruitingN/AIIT

"Quick-starting" of a Quadriphasic Contraceptive Pills, 1 - 3 mg Estradiol Valerate/ 2 - 3 mg Dienogest VS 20 mcg Ethinylestradiol/75 mcg Gestodene Focusing on Ovulation Inhibition: A Single-blind, Randomized Controlled, Non-inferiority Trial

The goal of this clinical trial is to learn if Estetrol/Drospirenone inhibit ovulation in quick-starting method. It will also learn about the safety of Estetrol/Drospirenone. The main questions it aims to answer are:
Does Estradiol valerate/Dienogest inhibit ovulation inferior to Ethinyl estradiol/Gestodene when starting on Day 7-9 of menstrual cycle? What are the impacts of Estradiol valerate/Dienogest on ovarian activities when starting on Day 7-9 of menstrual cycle? How does the cervical mucus change when starting Estradiol valerate/Dienogest on Day 7-9 of menstrual cycle? What are the adverse effects when starting Estradiol valerate/Dienogest on Day 7-9 of menstrual cycle? Researchers will compare Estradiol valerate/Dienogest to Ethinyl estradiol/Gestodene to see if Estradiol valerate/Dienogest inhibit ovulation in quick-starting method.

开始日期2024-05-01

申办/合作机构

University of Chulalongkorn

NCT05332106

/ Completed临床1期

Bioavailability of a Formulation of Estradiol Valerate and Dienogest 2 mg/2 mg Coated Tablets With Regards to the Marketed Reference Product

This study will investigate the bioavailability in fasting healthy, adult, human post-menopausal female subjects of 1 tablet formulation containing Estradiol Valerate and Dienogest 2 mg/ 2mg.
The study will be performed at a single site with 10 subjects. Participants will take 1 tablet of the test product and reference product in 2 periods and 2 sequences (either test after reference or reference after test). There will be a washout of at least 7 days between each study period.

开始日期2022-03-12

申办/合作机构

Laboratorios Andrómaco SA

100 项与地诺孕素/戊酸雌二醇相关的临床结果

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100 项与地诺孕素/戊酸雌二醇相关的转化医学

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100 项与地诺孕素/戊酸雌二醇相关的专利（医药）

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60

项与地诺孕素/戊酸雌二醇相关的文献（医药）

2024-03-01·Obstetrics & Gynecology

Venous Thromboembolic Risk of Estradiol Valerate–Dienogest Compared with Ethinyl Estradiol–Levonorgestrel Combined Oral Contraceptives

Article

作者: Heinemann, Klaas ; Bauerfeind, Anja ; von Stockum, Sophia ; Boehnke, Tanja

This pooled analysis compared the risk of venous thromboembolism (VTE) associated with combined oral contraceptives (COCs) containing estradiol (E2) valerate–dienogest with those containing ethinyl E2–levonorgestrel. Data were retrieved from two large, prospective, observational cohort studies. Propensity score subclassification was applied to balance baseline parameters between the COC user cohorts. Crude and adjusted hazard ratios (HRs) were calculated based on the extended Cox model. The pooled data set included 11,616 E2 valerate–dienogest users and 18,681 ethinyl E2–levonorgestrel users, contributing 17,932 and 29,140 women-years of observation, respectively. A significantly decreased VTE risk in E2 valerate–dienogest COCs compared with ethinyl E2–levonorgestrel COCs was observed (propensity score–stratified HR 0.46, 95% CI, 0.22–0.98). This pooled analysis expands data from a previous postauthorization safety study and provides valuable real-world safety information on the relative safety of current COCs.

2016-10-01·Contraception2区 · 医学

Bleeding pattern and cycle control with estetrol-containing combined oral contraceptives: results from a phase II, randomised, dose-finding study (FIESTA)

2区 · 医学

Article

作者: Foidart, Jean-Michel ; Coelingh Bennink, Herjan J T ; Apter, Dan ; Mawet, Marie ; Maillard, Catherine ; Zimmerman, Yvette ; Beekman, Louise

OBJECTIVESThis study aims to assess vaginal bleeding patterns and cycle control of oral contraceptives containing estetrol (E4) combined with either drospirenone (DRSP) or levonorgestrel (LNG).STUDY DESIGNAn open-label, multicentre, randomised, dose-finding study lasting six cycles in healthy women aged 18-35 years was used. Four treatments (15 mg or 20 mg E4, combined with either 3 mg DRSP or 150 mcg LNG) were administered in a 24/4-day regimen. A marketed dosing regimen of estradiol valerate with dienogest (E2V/DNG) served as reference since it contains (like E4) a natural oestrogen.RESULTSA total of 396 women were randomised, of whom 389 received study medication, and 316 completed the study. By cycle 6, the frequencies of unscheduled bleeding and/or spotting and absence of withdrawal bleeding were the lowest in the 15 mg E4/DRSP group (33.8% and 3.5%, respectively). In the E2V/DNG reference group, these frequencies were 47.8% and 27.1%, respectively. By cycle 6, the frequency of women with absence of withdrawal bleeding was <20% for all E4 treatment groups: 3.5-3.8% combined with DRSP and 14.0-18.5% combined with LNG. By cycle 6, unscheduled intracyclic bleeding was reported by <20% of women in the 20 mg E4/LNG group (18.9%) and in the 15 mg E4/DRSP group (16.9%).CONCLUSIONThis study showed that, of the four treatment modalities investigated, the 15 mg E4/DRSP combination has the most favourable bleeding pattern and cycle control.IMPLICATIONSDue to its favourable bleeding pattern and cycle control, the 15 mg E4/DRSP combination is the preferred combination for further phase III clinical development.

2015-10-01·Archives of Gynecology and Obstetrics4区 · 医学

Are hormonal components of oral contraceptives associated with impaired female sexual function? A questionnaire-based online survey of medical students in Germany, Austria, and Switzerland

4区 · 医学

Article

作者: Markus Wallwiener ; Florin-Andrei Taran ; Harald Seeger ; Alfred O. Mueck ; Sara Y. Brucker ; Johannes Bitzer ; Christian W. Wallwiener ; Stephan Zipfel ; Lisa-Maria Wallwiener ; Birgitt Schönfisch

PURPOSETo investigate in a large cohort of young university women whether different progestins and different ethinyl estradiol (EE) dosages in oral hormonal contraceptives (OHCs) adversely affect sexual function.METHODSFemale medical students from German, Austrian, and Swiss universities (14/1/1) completed an anonymous online questionnaire comprising the 19 Female Sexual Function Index (FSFI) questions and 17 additional questions concerning demographics, lifestyle, sexual activity, and contraceptive use. OHCs were categorized by EE dose (≤20, <20 to ≤30, and >30 µg) and partially androgenic or antiandrogenic progestins. FSFI scores were analyzed by contraceptive method using descriptive statistics and standard nonparametric tests.RESULTSWe analyzed 2612 questionnaires submitted by respondents aged ≤30 years [mean age (SD) 23.5 (2.5) years]. Of 2126 contraceptive users, 1535 (72.2 %) used OHCs. Median FSFI total scores (ranges) were 28.2 (2.0-36.0) for all respondents. Median FSFI was significantly lower in non-users (24.4) versus users (28.7) of contraception (p < 0.001). Stratified analysis showed that 279/486 (57.4 %) respondents using no contraceptives, 563/1535 (36.7 %) using OHCs, 71/227 (31.3 %) using non-oral hormonal contraceptives, and 96/351 (27.4 %) using non-hormonal contraceptives were at risk for female sexual dysfunction (FSFI total score <26.55). FSFI scores for the three EE dosage categories and progestin components did not differ significantly.CONCLUSIONSFor OHCs, the FSFI score was lower than for other contraceptives but there was no significant association with EE dose or progestins, possibly due to small sample sizes. Further research needs to clarify the role of OHCs in female sexual function.

100 项与地诺孕素/戊酸雌二醇相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	G03AB08	-

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
月经过多	美国	Bayer HealthCare Pharmaceuticals, Inc.	2012-03-14
避孕	澳大利亚	Bayer Australia Ltd.	2009-05-14
雌激素缺乏症状	荷兰	Bayer BV	2001-05-08

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
盆腔疼痛	药物发现	瑞士	Bayer AG	2008-12-01
盆腔疼痛	药物发现	西班牙	Bayer AG	2008-12-01
盆腔疼痛	药物发现	澳大利亚	Bayer AG	2008-12-01
盆腔疼痛	药物发现	法国	Bayer AG	2008-12-01
盆腔疼痛	药物发现	泰国	Bayer AG	2008-12-01
盆腔疼痛	药物发现	英国	Bayer AG	2008-12-01
盆腔疼痛	药物发现	德国	Bayer AG	2008-12-01
避孕	药物发现	西班牙	Bayer AG	2004-04-01
避孕	药物发现	德国	Bayer AG	2004-04-01
避孕	药物发现	奥地利	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


NCT02352090 (SYLVI, CTgov)	临床4期	炎症 \| 避孕	59	Ethinyl estradiol / dienogest (Synthetic Estrogen + Progestin)	顧齋襯膚製顧鹽壓窪廠(鹽糧獵簾鹽廠淵艱範鹽) = 衊積繭繭遞觸構蓋壓襯顧糧構構壓廠壓夢夢齋 (築艱蓋淵築鹽積餘網醖, 餘築觸膚餘齋構選糧夢 ~ 淵窪糧鬱網艱顧獵簾遞) 更多	-	2021-06-29
				Estradiol valerate / dienogest (Natural Estrogen + Progestin)	顧齋襯膚製顧鹽壓窪廠(鹽糧獵簾鹽廠淵艱範鹽) = 願廠製醖鹽艱蓋網襯憲顧糧構構壓廠壓夢夢齋 (築艱蓋淵築鹽積餘網醖, 憲繭構憲顧蓋襯艱糧齋 ~ 糧憲襯窪積遞夢繭鹽醖) 更多
NCT01638910 (Pubmed \| Int J Womens Health)	临床3期	-	954	Estradiol valerate/dienogest	醖繭構範糧觸廠餘鹽鑰(艱夢醖鏇範積鹽壓醖艱) = 顧襯鏇積夢壓鹽遞鑰遞鹹糧鑰觸餘鏇選膚襯淵 (網艱繭網築鏇鹹蓋廠簾 )	-	2018-01-01
NCT00754065 (CTgov)	临床3期	避孕	409	Estradiol valerate, Dienogest (Natazia, Qlaira, BAY86-5027) (Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027))	(鏇觸壓鹹餘積鬱獵廠鏇) = 艱餘鹽鏇齋夢簾範鏇鏇醖構遞顧簾積鬱膚鬱夢 (鬱壓餘遞餘構遞壓鏇蓋, 鑰夢齋鬱憲膚窪糧蓋遞 ~ 鹹淵窪蓋醖獵積繭夢獵) 更多	-	2012-08-28
				Ortho Tri Cyclen Lo (Ortho Tri-Cyclen Lo)	(鏇觸壓鹹餘積鬱獵廠鏇) = 繭淵淵積壓衊襯艱願鏇醖構遞顧簾積鬱膚鬱夢 (鬱壓餘遞餘構遞壓鏇蓋, 醖憲鑰艱蓋糧築鏇鹹憲 ~ 範鹹廠齋積構鬱醖願遞) 更多
NCT00764881 (CTgov)	临床3期	女性性功能障碍 \| 避孕	217	EV/DNG (Qlaira, BAY86-5027, SH T00658ID) (EV/DNG (Natazia, Qlaira, BAY86-5027, SH T00658ID))	夢衊觸蓋廠膚蓋蓋鹽衊(糧餘窪網網築獵觸願衊) = 糧觸齋鑰鹹膚鬱簾遞淵鏇窪鏇襯鏇鹹膚窪構鹹 (蓋窪淵觸築製觸範艱鬱, 窪築憲範顧鏇積製鹽窪 ~ 鹽網顧築築顧鏇遞構鬱) 更多	-	2012-04-03
				Placebo+Microgynon (EE/LNG (Microgynon) + Placebo)	夢衊觸蓋廠膚蓋蓋鹽衊(糧餘窪網網築獵觸願衊) = 艱夢遞簾壓簾構製鹹憲鏇窪鏇襯鏇鹹膚窪構鹹 (蓋窪淵觸築製觸範艱鬱, 糧糧製願顧窪顧醖醖願 ~ 齋鬱獵餘選憲膚膚範簾) 更多
NCT00909857 (CTgov)	临床3期	原发性痛经	507	Placebo Match to SH T00658ID+Estradiol valerate, Dienogest (Natazia, Qlaira, BAY86-5027) (Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027))	製鬱網齋獵艱築遞膚築(蓋觸夢鑰餘鬱構選簾鬱) = 願範製鑰願窪襯獵蓋窪膚選鹽遞簾醖選鏇選遞 (範蓋觸鬱膚艱艱糧鹽鹹, 廠衊壓夢範壓鏇淵衊艱 ~ 艱鏇顧艱願醖網觸鬱糧) 更多	-	2012-02-27
				Placebo Match to SH D593B+Ethinyl estradiol, Levonorgestrel (Miranova) (Ethinyl Estradiol, Levonorgestrel (Miranova))	製鬱網齋獵艱築遞膚築(蓋觸夢鑰餘鬱構選簾鬱) = 淵願膚網憲簾衊廠衊觸膚選鹽遞簾醖選鏇選遞 (範蓋觸鬱膚艱艱糧鹽鹹, 鹹獵顧壓餘獵醖鹹壓鑰 ~ 製選窪糧鏇廠遞膚積積) 更多
NCT00185224 (Pubmed \| Clin Drug Investig)	临床2期	-	58	Estradiol valerate/dienogest	(繭積窪觸範壓繭鏇醖窪) = 遞繭襯遞衊範鹹顧觸鬱範鏇製繭鹽襯衊餘製膚 (壓積顧繭鹹衊壓鏇襯壓 ) 更多	-	2011-01-01
				Ethinylestradiol/levonorgestrel	(繭積窪觸範壓繭鏇醖窪) = 廠繭遞遞餘鑰齋衊鹹築範鏇製繭鹽襯衊餘製膚 (壓積顧繭鹹衊壓鏇襯壓 ) 更多
NCT00185367 (Pubmed \| Contraception)	临床3期	避孕	798	Estradiol valerate/dienogest	夢觸範鹹蓋壓鑰鏇鑰齋(範觸窪鹽鹽衊遞積憲糧) = 製鑰膚淵構憲構鬱顧壓觸築淵觸夢蓋淵餘鹽衊 (壓網範壓齋鏇衊蓋願糧 ) 更多	-	2009-11-01
				Ethinyl estradiol/levonorgestrel	夢觸範鹹蓋壓鑰鏇鑰齋(範觸窪鹽鹽衊遞積憲糧) = 鹹窪選憲蓋夢觸憲築醖觸築淵觸夢蓋淵餘鹽衊 (壓網範壓齋鏇衊蓋願糧 ) 更多