地诺孕素/炔雌醇(Ethinyl Estradiol/Dienogest) - 药物靶点：ER x PR_在研适应症：成人痤疮，避孕_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Valette

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

皮肤和肌肉骨骼疾病其他疾病

在研适应症

成人痤疮避孕

非在研适应症-

原研机构

Jenapharm GmbH & Co. KG

在研机构

Bayer Australia Ltd.

Jenapharm GmbH & Co. KG

Insud Pharma SL

非在研机构

Bayer AG

最高研发阶段批准上市

首次获批日期

澳大利亚 (2006-03-02),

成人痤疮避孕

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C40H49NO4

InChIKeyJRGZBMMCVMDOKI-DHLNHIIISA-N

CAS号170475-05-5

关联

8

项与地诺孕素/炔雌醇相关的临床试验

NCT06316206

/ Completed临床4期IIT

The Use of Ethinylestradiol/Dienogest in Random Start Rapid Preparation of Endometrium Before Office Hysteroscopic Polypectomies: a Multicenter, Prospective, Randomized Study

The presence of a thin endometrium plays an important role in enabling the best conditions for hysteroscopic surgery. Recently, for this purpose, many studies have evaluated the effect of preoperative administration of a variety of drugs. We explored the efficacy of random started 14-day administration of Ethinylestradiol/Dienogest, in rapid preparation of endometrium for hysteroscopic polypectomy.

开始日期2023-01-01

申办/合作机构

University of Palermo

[+1]

NCT06324851

/ Completed临床4期IIT

The Use of Drospirenone/Estetrol, Nomegestrol Acetate/Estradiol and Ethinylestradiol/Dienogest in Random Start Rapid Preparation of Endometrium Before Office Hysteroscopic Polypectomies: a Multicenter, Prospective, Randomized Study

The presence of a thin endometrium plays an important role in enabling the best conditions for hysteroscopic surgery. Recently, for this purpose, many studies have evaluated the effect of preoperative administration of a variety of drugs. We explored the efficacy of random started 14-day administration of Drospirenone/Estetrol or Nomegestrol Acetate/Estradiol or Ethinylestradiol/Dienogest, in rapid preparation of endometrium for hysteroscopic polypectomy.

开始日期2023-01-01

申办/合作机构

University of Palermo

[+1]

NCT03945513

/ Completed临床3期

A Multicenter, Non-Comparative Trial on the Contraceptive Efficacy, Safety, and Tolerability of LPRI-424 (Dienogest 2 mg / Ethinyl Estradiol 0.02 mg) During 13 Cycles

The main objective of this trial is to demonstrate the contraceptive efficacy of LPRI424, Additional goals of the trial are to demonstrate the safety and tolerability of LPRI424.

开始日期2019-12-03

申办/合作机构

Insud Pharma SL

[+1]

100 项与地诺孕素/炔雌醇相关的临床结果

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100 项与地诺孕素/炔雌醇相关的转化医学

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100 项与地诺孕素/炔雌醇相关的专利（医药）

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29

项与地诺孕素/炔雌醇相关的文献（医药）

2024-05-03·Chronobiology International

Menstrual cycle phases and dosage of synthetic hormonal contraceptives influence diurnal rhythm characteristics of distal skin temperature

Article

作者: Möllgaard, Leefke ; Engelhard, Felicia ; Dittmar, Manuela

This study aimed to explore how natural menstrual cycle phases and dosage of oral hormonal contraceptives (OC) influence the diurnal rhythm of distal skin temperature (DST) under real-life conditions. Participants were 41 healthy females (23.9 ± 2.48 y), comprising 27 females taking monophasic hormonal oral contraceptives (OC users) and 14 females with menstrual cycles (non-OC users). Wrist DST was continuously recorded and averaged over two consecutive 24-hour days during (pseudo)follicular and (pseudo)luteal menstrual phases. Diurnal rhythm characteristics, i.e. acrophase and amplitude, describing timing and strength of the DST rhythm, respectively, were calculated using cosinor analysis. Results show that non-OC users experienced earlier diurnal DST maximum (acrophase, p = 0.019) and larger amplitude (p = 0.016) during the luteal phase than during the follicular phase. This was observed in most (71.4%) but not all individuals. The OC users showed no differences in acrophase or amplitude between pseudoluteal and pseudofollicular phases. OC users taking a higher dosage of progestin displayed a larger amplitude for DST rhythm during the pseudoluteal phase (p = 0.009), while estrogen dosage had no effect. In conclusion, monophasic OC cause changes in diurnal DST rhythm, similar to those observed in the luteal phase of females with menstrual cycles, suggesting that synthetic progestins act in a similar manner on skin thermoregulation as progesterone does.

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.

2012-03-01·Diabetic Medicine2区 · 医学

Oral contraception enhances growth hormone responsiveness to hyper‐ and hypoglycaemia

2区 · 医学

Article

作者: M. Loebig ; K. Jauch-Chara ; K. Diedrich ; S. Tauchert ; A. K. Ludwig ; S. Rudolf ; K. M. Oltmanns ; U. Schweiger ; A. Friedrich

Diabet. Med. 29, 345–350 (2012)AbstractAims Plasma glucose levels influence growth hormone concentrations. Oral contraceptives are known to affect circulating growth hormone levels and glucose metabolism. While growth hormone plays an important role in hypoglycaemia counter‐regulation, it has been shown that oral contraceptives increase growth hormone concentrations. In this context, we tested if serum growth hormone concentrations display a differential response on glycaemic variations in healthy women using oral contraceptives and those not using contraceptives.Methods Fifteen healthy women with oral contraceptive treatment and 10 without participated in a stepwise hyper‐ and hypoglycaemic glucose clamp procedure. Serum growth hormone concentrations were measured at euglycaemic baseline and subsequently at plasma glucose plateaus of 8.8, 6.8, 4.8 and 2.8 mmol/l.Results Growth hormone values were significantly higher in women using oral contraceptives throughout the experiments (P = 0.001). Hyperglycaemia decreased growth hormone concentrations in women using oral contraceptives (P = 0.009), but not in those who were not using oral contraceptives (P = 0.241). Hypoglycaemia significantly elevated growth hormone concentrations in women using oral contraceptives (P = 0.009), but not in those not using oral contraceptives (P = 0.094). Maximum growth hormone values were reached at the end of the hypoglycaemic plateau, with significantly higher concentrations in the group using oral contraceptives than in the group not using oral contraceptives (P = 0.016).Conclusion Healthy women on oral contraceptive treatment display an increased responsiveness of growth hormone to hypoglycaemic, as well as hyperglycaemic conditions and generally higher serum growth hormone concentrations than women without oral contraceptives. Given the known boosting effects of growth hormone on hypoglycaemic hormonal counter‐regulation, oral contraceptives may thus be a pharmacological candidate contributing to combat hypoglycaemia unawareness in women with diabetes in the future.

100 项与地诺孕素/炔雌醇相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
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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
成人痤疮	澳大利亚	Bayer Australia Ltd.	2006-03-02
避孕	-	Jenapharm GmbH & Co. KG	-

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
寻常痤疮	药物发现	乌克兰	Bayer AG	2004-03-10
寻常痤疮	药物发现	俄罗斯	Bayer AG	2004-03-10
寻常痤疮	药物发现	斯洛伐克	Bayer AG	2004-03-10
寻常痤疮	药物发现	波兰	Bayer AG	2004-03-10
寻常痤疮	药物发现	捷克	Bayer AG	2004-03-10
避孕	药物发现	德国	Bayer AG	2003-06-01

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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)	憲鏇製觸製願膚壓艱製(顧壓鹹遞廠範憲襯壓鏇) = 選願窪構淵繭衊顧醖顧遞顧鹹簾繭繭廠鏇繭窪 (憲衊艱選範衊衊鹽獵顧, 顧遞襯窪願艱鬱鑰壓艱 ~ 繭範顧夢窪鏇襯窪壓鏇) 更多	-	2021-06-29
				Estradiol valerate / dienogest (Natural Estrogen + Progestin)	憲鏇製觸製願膚壓艱製(顧壓鹹遞廠範憲襯壓鏇) = 廠糧築夢鑰蓋襯選醖選遞顧鹹簾繭繭廠鏇繭窪 (憲衊艱選範衊衊鹽獵顧, 觸遞糧艱鏇築齋衊簾積 ~ 艱窪網觸鹽蓋艱艱壓壓) 更多