地诺孕素/炔雌醇(Ethinyl Estradiol/Dienogest) - 药物靶点：ER x PR_在研适应症：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

其他疾病

在研适应症

避孕

非在研适应症-

原研机构

Jenapharm GmbH & Co. KG

在研机构

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-

最高研发阶段(中国)-

特殊审评-

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结构

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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6

项与地诺孕素/炔雌醇相关的文献（医药）

2003-01-01·British Journal of Clinical Pharmacology

Unwanted pregnancy on self‐medication with St John's wort despite hormonal contraception

Letter

作者: W. Kirch ; Barbara Büschel ; Ute I. Schwarz

Many patients take St John's wort (SJW, Hypericum perforatum), a herbal remedy, to treat symptoms of depression, often without the knowledge of their physician. Widely available without prescription, it is considered by some to be a safe because it is a ‘natural’ alternative to more traditional antidepressants. Recent reports indicate that SJW has been implicated in numerous herb–drug interactions that may have clinical significance [1]. Women taking oral contraceptives and SJW have reported breakthrough menstrual bleeding, but this is the first published case of an unexpected pregnancy in association with SJW consumption [2]. A 36-year-old woman with depression and hypercholesterolaemia presented to a gynaecology practice with an unexpected pregnancy confirmed by ultrasound. the drug history revealed regular use of the combined oral contraceptive Valette® (ethinyl oestradiol/dienogesterol) over the last year. She had been treated with fluvastatin (20 mg day−1) for 2 years, and with different antidepressants including selective serotonin reuptake inhibitors and tricyclic antidepressants after an attempted suicide in 1995. the patient began self-medicated with the over-the-counter Hypericum extract Helarium®425 (Bionorica) with daily doses up to 1700 mg approximately 3 months prior to conception, and until conception no other medication was taken except the hormonal contraceptive. aA therapeutic abortion was carried out and revealed a healthy, 17-week-old, 144 g male foetus. Co-administration of SJW has resulted in markedly reduced blood levels of drugs such as cyclosporin, indinavir, and digoxin. Lowered levels of cyclosporin have contributed to the rejection of transplanted organs [3]. in healthy volunteers, 10–14 days of concomitant SJW resulted in 81% reduction of indinavir trough and 30% reduction of plasma digoxin concentrations [4, 5]. This effect is likely mediated through induction of the drug metabolizing enzyme cytochrome P450 3a (CYP3a) and the efflux transporter P-glycoprotein that is encoded by the multidrug resistance gene MDR1[6]. Hyperforin, a major phytochemical present in SJW, is a potent activator of the human nuclear receptor pregnane X (PXR) [7]. Both CYP3A4 and MDR1 have PXR response elements in their 5′-upstream regulatory regions, and activation will lead to enhanced expression of the encoded proteins [8, 9]., Clinical studies with the antibiotic rifampin, like SJW a potent inducer of CYP3a and P-glycoprotein, have demonstrated a significant decrease of the mean AUC of ethinyl estradiol and norethindrone in healthy women [9, 10]. As the steroid hormone estradiol is subject to P-glycoprotein- efflux and CYP3a metabolism, induction can lead to enhanced elimination of the hormone that would lead to ineffective contraception [11, 12]. Four other cases of ineffective contraception coincident with SJW consumption have been reported to the German authorities (German Federal Institute for Drugs and Medical Devices, Drug Commission of the German Medical Profession). Because of this pharmacokinetic interaction, alternative methods of contraception are strongly recommended when SJW is used. Accurate information regarding drug interactions and the potential failure of oral contraceptives should be provided to consumers of SJW. Thus far, product information accompanying Hypericum extracts does not adequately describe the potential risk for herb–drug interactions.

2001-04-01·Die Pharmazie

Non-protein bound dienogest in serum and salivary dienogest in women taking the oral contraceptives Certostat and Valette.

Article

作者: Schön, R ; Hobe, G ; Jäger, R ; Küntzel, B ; Piater, T ; Klinger, G

Dienogest (17 alpha-cyanomethyl-17-hydroxy-4,9-estradien-3-one) is the progestagen component of the oral contraceptives Certostat and Valette. In contrast to other 19-norsteroid progestagens like levonorgestrel, norethisterone, gestodene and 3-ketodesogestrel, dienogest does not bind to sexual hormone binding globulin (SHBG). The absent binding to SHBG results in a high portion of free, non-protein bound dienogest in serum. In female volunteers taking the oral contraceptives Certostat and Trisiston, the part of non-protein bound dienogest and levonorgestrel, respectively, in serum was determined by the method of centrifugal ultrafiltration. The portion of free dienogest was found to be 9.55 +/- 0.95% (m +/- SD, n = 13) of total serum dienogest. Free levonorgestrel constituted 0.97 +/- 0.14% (n = 12) of total serum levonorgestrel. In an investigation with 47 female volunteers taking Certostat, serum total dienogest was quantified by a specific radioimmunoassay and free dienogest in serum by centrifugal ultrafiltration. In the serum samples with dienogest concentrations in the range of 4.1-57.7 ng/ml, the part of free, non-protein bound dienogest was found to be 8.90 +/- 0.54% of serum total dienogest. There is a high correlation between serum total dienogest and free dienogest (r = 0.989). In another investigation with 20 female volunteers taking the contraceptive Valette, serum total dienogest and salivary dienogest were quantified by radioimmunoassay and free dienogest in serum by centrifugal ultrafiltration. In the serum samples with dienogest concentrations in the range of 7.5-50.6 ng/ml, the part of free, non-protein bound dienogest was 8.78 +/- 0.77% of serum total dienogest. Salivary dienogest constituted 7.99 +/- 0.94% of serum total dienogest showing a high correlation with serum free dienogest (r = 0.953) and serum total dienogest (r = 0.958). The high portion of non-protein bound compound in serum is a characteristic pharmacokinetic feature of dienogest.

2000-06-01·Journal of Clinical Pharmacy and Therapeutics4区 · 医学

Effect of oral contraceptives on the urinary excretion of biochemical markers indicating vasoactive action

4区 · 医学

Article

作者: Wallwiener D ; Gräser T ; Mueck Ao ; Lüdtke R ; Seeger H

OBJECTIVEIn the present study the effect of two contraceptive pills, i.e. Neorlest, containing ethinylestradiol and norethisterone acetate, and Valette, containing ethinylestradiol and the new progestin dienogest, was investigated on the urinary excretion of vasoactive markers. As markers prostacyclin and its antagonist thromboxane, cGMP, serotonin, and the vasorelaxing mediators relaxin and urodilatin were measured.METHOD30 women received Neorlest and 33 women Valette in a randomized, open, parallel-group study design. Nocturnal urine was collected before treatment and during cyclic treatment after 6 and 11 weeks.RESULTSFor prostacyclin, the ratio of prostacyclin to thromboxane, relaxin and urodilatin significant increases compared to the pretreatment values were observed with Valette within 11 weeks treatment. For the markers cGMP and serotonin both contraceptive pills showed a tendency to an increase of the renal excretion after 11 weeks treatment. No significant differences between the two pills were observed, except in the case of the ratio of prostacyclin to thromboxane, which showed a significant, clear-cut enhancement with Valette.CONCLUSIONThese results indicate that contraceptive pills may stimulate the production of vasodilative markers, an effect which can be attributed most likely to the oestrogenic component of the pill. The progestogenic component of the pill may elicit an impact on this oestrogen-induced vasodilation, which, however, seems to be minimized in the case of the new compound dienogest, a C-19 progestin with antiandrogenic properties.

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

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适应症	国家/地区	公司	日期
避孕	-	Jenapharm GmbH & Co. KG	-

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适应症	最高研发状态	国家/地区	公司	日期
避孕	临床3期	美国	Insud Pharma SL	2019-12-03

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临床结果

适应症

分期

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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)	顧鹹遞艱窪鬱製廠廠願(觸構襯衊選網廠構鏇襯) = 鑰選糧窪構膚醖鑰醖窪窪襯鬱壓繭網齋憲壓夢 (築廠窪願壓繭憲餘憲鏇, 鑰廠淵觸網鏇壓顧顧獵 ~ 壓衊顧醖糧鏇選憲艱醖) 更多	-	2021-06-29
				Estradiol valerate / dienogest (Natural Estrogen + Progestin)	顧鹹遞艱窪鬱製廠廠願(觸構襯衊選網廠構鏇襯) = 窪醖衊鹹構繭憲糧醖選窪襯鬱壓繭網齋憲壓夢 (築廠窪願壓繭憲餘憲鏇, 顧網築選廠顧鬱繭願夢 ~ 廠襯鬱廠範繭艱繭餘構) 更多