雌二醇/左炔诺孕酮(Estradiol/Levonorgestrel) - 药物靶点：ER x PR_在研适应症：绝经期后骨质疏松，血管疾病，血管舒缩症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Climara Pro、Fem7 Combi

+ [3]

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

心血管疾病内分泌与代谢疾病皮肤和肌肉骨骼疾病

在研适应症

绝经期后骨质疏松血管疾病血管舒缩症

非在研适应症-

原研机构

Bayer AG

在研机构

Berlex Laboratories, Inc.

Bayer HealthCare Pharmaceuticals, Inc.

Bayer Yakuhin Ltd.

+ [1]

非在研机构-

权益机构-

最高研发阶段批准上市

首次获批日期

美国 (2003-11-21),

血管舒缩症

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C39H52O4

InChIKeyRQFMPXMLRRPOJH-ORADRBJOSA-N

CAS号88873-29-4

关联

7

项与雌二醇/左炔诺孕酮相关的临床试验

NCT06455969

/ Recruiting临床4期IIT

Musculoskeletal Resiliency and Adaptation to Sex Steroid Suppression and Replacement During Multi-Stressor Training

Non-combat-related muscle, tendon and bone injuries are the most common injuries suffered by military personnel, particularly in new recruits. These injuries impact military readiness and are responsible for roughly 60% of limited duty days, 65% of soldiers who are unable to deploy, and nearly $500 million in medical cost to the government annually in the Army alone. Drug interventions must be studied and developed to prevent these negative outcomes and prepare military personnel for the demands of military service. At the current time, military leadership has identified critical gaps in understanding how to minimize these injuries and train soldiers with drug intervention serving among those gaps.
The goal of this study is to determine how a hormonal intervention can change muscle, tendon, and bone function as well as physical and psychological performance in response to mental and physical stress. To do so, we will examine sex hormone (testosterone, estrogen) levels, muscle, tendon, and bone images, blood samples, and physical and mental performance. We will look at things like changes in hormone levels, chemicals released from active skeletal muscles, and your body composition. The results from this study will be used to improve physical readiness training in the military with the goal of reducing injuries.

开始日期2024-07-15

申办/合作机构

University of Pittsburgh

[+1]

NCT02393482

/ Unknown status临床4期IIT

Psychological Impact of Amenorrhea in Women With Endometriosis: Perspective Randomized Study

The purpose of the study is to evaluate the impact on quality of life, psychological health, sexuality and chronic pain of therapies which determine amenorrhea in symptomatic women with endometriosis, through the administration of self reported questionnaires. Amenorrhea in the first group is caused by balanced assumption of estroprogestins, in the second group is caused by GnRHa-induced hypoestrogenism.

开始日期2021-06-01

申办/合作机构

University of Cagliari

NCT02475265

/ Completed临床2期IIT

Transdermal Estrogen in Older Premenopausal Women With Anorexia Nervosa

Decreased bone strength is a common and serious medical problem present in many women with anorexia nervosa. Women with decreased bone strength are more likely to suffer broken bones than women with normal bone strength.
This study will investigate whether the use of transdermal estrogen can improve bone mineral density (BMD) and bone microarchitecture in women with anorexia nervosa anorexia nervosa when used for 6 months.

开始日期2015-07-01

申办/合作机构

The General Hospital Corp.

[+1]

100 项与雌二醇/左炔诺孕酮相关的临床结果

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100 项与雌二醇/左炔诺孕酮相关的转化医学

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100 项与雌二醇/左炔诺孕酮相关的专利（医药）

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32

项与雌二醇/左炔诺孕酮相关的文献（医药）

2012-06-01·Hormone and Metabolic Research4区 · 医学

Proliferative Effects of Estradiol- or Ethinylestradiol-Progestogen Combinations on Human Breast Cancer Cells in an Intermitted and a Long-term Regimen

4区 · 医学

Article

作者: Mueck, A. ; Merki-Feld, G. ; Seeger, H.

Currently the use of natural estradiol as estrogenic component in oral contraceptives is more and more extended. It is unknown whether the application of this estrogen is associated with a different breast cancer risk as compared to the common use of the synthetic ethinylestradiol. In addition with the intention to reduce menstruation associated symptoms and bleeding periods an extended-cycle regimen is currently considered. In the present in vitro work, we have compared the effect of these different estrogenic compounds and the different treatment regimens on breast cancer risk. Human breast cancer cells (ZR75-1 and HCC1500) were incubated with equimolar concentrations of estradiol or ethinylestradiol combined with various progestogens, dienogest, drospirenone, keto-desogestrel, levonorgestrel, and nomegestrel. Usual and extended cycle was mimicked by incubation periods of 3 days with 1 day hormones off and 4 days, respectively. Molecular markers for proliferation and apoptosis were investigated by Western blot. In both cell lines estradiol and ethinylestradiol elicited a significant increase in the proliferation rate without difference between the 2 estrogens. The effect in the long-term cycle tended to be more pronounced than in the intermitted cycle. Progestogen addition most significantly reduced the estrogen-induced proliferation rate. The molecular markers were influenced by the progestogens mostly in the same manner, reducing the proliferation/apoptosis rate. Our results indicate that both estrogenic based combinations with progestogens may not increase breast cancer risk independent from the regimen, intermitted or long-term cycle. However clinical studies are necessary to prove these in vitro results.

2006-04-01·Life Sciences3区 · 医学

Cardiovascular, anthropometric and neurocognitive features of healthy postmenopausal women: Effects of hormone replacement therapy

3区 · 医学

Article

作者: Valeria Guazzoni ; Enrico Gabellieri ; Spyridon Chytiris ; Flavia Magri ; Lorena Busconi ; Ettore Ferrari ; Valeria Valdes ; Luca Cravello ; Anna Rita Sorrentino

Randomized clinical trials have not shown long-term benefit of postmenopausal hormone replacement therapy (PHT) nor have they shown conclusively that the harmful consequences outweighs the benefits of the treatment. Rather, it is possible that an individualized hormone replacement therapy in questionably clinically healthy postmenopausal women may lead to different results than randomized trials.DESIGNIn this cross-sectional study we evaluated anthropometric parameters, body composition, serum lipids, blood pressure, heart rate variability (HRV) and neurocognitive functions in 39 healthy postmenopausal women PHT users or not users (n=13, age 53.0+/-3.3 and n=26, age=53.3+/-5.0 SD, respectively) as well as in 27 younger controls (ages=33.3+/-7.1).RESULTSDemographic parameters were similar in women PHT users and not users. Postmenopausal women showed a significantly increase of body mass index (BMI) as well as of waist circumference, compared to younger controls, but in PHT users the values of fat free mass were intermediate between the ones of not treated and younger women. The study of HRV showed a reduction in low frequency (LF) component (sympathetic modulation) during the day, and a reduction in high frequency (HF) component (parasympathetic modulation), particularly in postmenopausal women without PHT. PHT users were characterized by autonomic parameters intermediate between younger controls and age-matched women without PHT.CONCLUSIONSThe impact of PHT on the age-dependent changes of anthropometric features and body composition seems to be modest but positive. Furthermore, PHT seems to play a positive role on the autonomic modulation of cardiac function, through a shift of LF/HF ratio values towards those of young controls.

2005-02-01·Maturitas3区 · 医学

Levonorgestrel and 17β-estradiol given transdermally for the prevention of postmenopausal osteoporosis

3区 · 医学

Article

作者: C. Christiansen ; P. Ravn ; L. Warming

AIMTo evaluate the efficacy and safety of a new transdermal continuous combined hormone replacement therapy (HRT) for the prevention of postmenopausal osteoporosis.METHODS212 osteopenic (lumbar spine and/or hip (femoral neck) bone mineral density (BMD) between -1.0 and -2.5 S.D. of the premenopausal mean value) postmenopausal women aged 45-65 years participated in a 2-year prospective study. Treatments were 45 microg 17beta-estradiol combined with 30 (n = 69) or 40 microg (n = 72) levonorgestrel daily or placebo (n = 71) given as a 7-day patch. All received a daily supplement of 500 mg calcium. BMD at lumbar spine (L2-L4), hip and total body, as well as blood and urinary biochemical markers of bone turnover (serum osteocalcin (sOC), serum bone-specific alkaline phosphatase (sBSAP), urinary calcium (uCa) and urinary CrossLaps (uCTX)) were measured regularly.RESULTSBMD at the lumbar spine, hip and total body increased by 8, 6 and 3% (P < 0.001), respectively, in the hormone groups versus placebo. The bone markers all decreased accordingly (sOC: 37%, sBSAP: 34% and uCTX: 65% from baseline (all P < 0.001)), except for uCa that did not change significantly. No significant dose-related effect of levonorgestrel was found. Vaginal bleeding/spotting decreased from 48 to 25% of the HRT-treated women during the study period. Skin tolerance was good in 84% of the women with no difference between the study groups. No incidences of endometrial hyperplasia, uterine or mammary cancer occurred.CONCLUSIONThe transdermal combination of 17beta-estradiol and levonorgestrel has a positive effect on BMD in an osteopenic postmenopausal population. Furthermore, a high safety profile was observed.

100 项与雌二醇/左炔诺孕酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	G03F	-

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
绝经期后骨质疏松	美国	Berlex Laboratories, Inc.	2005-12-27
血管疾病	美国	Schering AG	2005-12-27
血管舒缩症	美国	Bayer HealthCare Pharmaceuticals, Inc.	2003-11-21

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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


NCT02475265 (1180, CTgov)	临床2期	骨质疏松症 \| 神经性厌食症	11	estradiol 0.045 mg/levonorgestrel 0.015mg	構範網衊膚艱觸夢鑰範(構顧窪壓獵鏇糧鹹壓壓) = 範構餘鬱鏇構顧製襯繭網餘壓鹽遞選壓鬱獵選 (顧窪觸網鏇繭鬱蓋窪糧, 餘襯糧餘淵鬱獵襯廠醖 ~ 簾積艱遞構鏇蓋網構醖) 更多	-	2019-07-22