Delving into the Latest Updates on Drospirenone/Ethinyl Estradiol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Drospirenone/Ethinylestradiol Betadex, ドロスピレノン/エチニルエストラジオールベータデクス

+ [21]

Target

AR x ER x MR x PR

Action

antagonists, agonists

Mechanism

AR antagonists(Androgen Receptor antagonists), ERs agonists(Estrogen receptors agonists), MR antagonists(Mineralocorticoid receptor antagonists)

+ [1]

Therapeutic Areas

Nervous System DiseasesUrogenital DiseasesOther Diseases

Active Indication

DysmenorrheaEndometriosisPremenstrual Dysphoric Disorder+ [1]

Inactive Indication

Primary dysmenorrhea

Originator Organization

Bayer AG

Active Organization

Bayer HealthCare Pharmaceuticals, Inc.

Bayer AGLupin Australia Pty Ltd.

+ [2]

Inactive Organization

Bayer HealthCare AG

Bayer Pharma AG

Bayer Healthcare Co., Ltd.

+ [1]

Drug Highest PhaseApproved

First Approval Date

Netherlands (08 Aug 2000),

Contraception

Regulation-

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Structure/Sequence

Molecular FormulaC44H54O5

InChIKeyJLQFVGYYVXALAG-CFEVTAHFSA-N

CAS Registry164017-31-6

主要研究目的：在健康受试者体内，空腹状态下，以Bayer Australia Ltd持证，Bayer Weimar GmbH und Co.KG生产的屈螺酮炔雌醇片（II）（商品名：优思悦，规格：屈螺酮3 mg和炔雌醇0.02 mg）为参比制剂，研究浙江爱生药业有限公司研制的屈螺酮炔雌醇片（II）（受试制剂，规格：炔雌醇0.020 mg和屈螺酮3.000 mg）的吸收速度和吸收程度，评价受试制剂与参比制剂是否具有生物等效性。次要研究目的：观察受试制剂和参比制剂在中国健康受试者中的安全性。

[Translation]

Main study objectives: In healthy subjects, under fasting conditions, using Drospirenone Ethinyl Estradiol Tablets (II) (trade name: Usile, specification: 3 mg drospirenone and 0.02 mg ethinyl estradiol) produced by Bayer Australia Ltd and Bayer Weimar GmbH und Co.KG as the reference preparation, to study the absorption rate and extent of Drospirenone Ethinyl Estradiol Tablets (II) (test preparation, specification: 0.020 mg ethinyl estradiol and 3.000 mg drospirenone) developed by Zhejiang Aisheng Pharmaceutical Co., Ltd., and to evaluate whether the test preparation and the reference preparation are bioequivalent. Secondary study objectives: Observe the safety of the test preparation and the reference preparation in healthy Chinese subjects.

Start Date13 Feb 2025

Sponsor / Collaborator

Zhejiang Aisheng Pharmaceutical Co. Ltd.

CTR20244534

/ CompletedNot Applicable

屈螺酮炔雌醇片在中国健康志愿者中空腹及餐后状态下的人体生物等效性试验

[Translation] Human bioequivalence study of drospirenone and ethinyl estradiol tablets in Chinese healthy volunteers under fasting and fed conditions

主要目的：研究空腹和餐后状态下单次口服受试制剂屈螺酮炔雌醇片（规格：每片含炔雌醇0.03mg和屈螺酮3mg，乐福思健康产业股份公司生产）与参比制剂屈螺酮炔雌醇片（优思明®，规格：每片含炔雌醇0.03mg和屈螺酮3mg；Bayer Australia Ltd持证，Bayer Weimar GmbH & Co. KG.生产）在健康成年受试者体内的药代动力学特征，评价空腹和餐后状态下口服两种制剂的生物等效性。次要目的：研究受试制剂屈螺酮炔雌醇片（规格：每片含炔雌醇0.03mg和屈螺酮3mg）和参比制剂屈螺酮炔雌醇片（优思明®）（规格：每片含炔雌醇0.03mg和屈螺酮3mg）在健康受试者中的安全性。

[Translation]

Primary objective: To study the pharmacokinetic characteristics of the test preparation drospirenone ethinyl estradiol tablets (specification: each tablet contains 0.03 mg ethinyl estradiol and 3 mg drospirenone, produced by Love Health Industry Co., Ltd.) and the reference preparation drospirenone ethinyl estradiol tablets (Yasmin®, specification: each tablet contains 0.03 mg ethinyl estradiol and 3 mg drospirenone; licensed by Bayer Australia Ltd, produced by Bayer Weimar GmbH & Co. KG.) in healthy adult subjects after single oral administration in fasting and fed state, and to evaluate the bioequivalence of the two preparations after oral administration in fasting and fed state. Secondary objective: To study the safety of the test preparation drospirenone ethinyl estradiol tablets (specification: each tablet contains 0.03 mg ethinyl estradiol and 3 mg drospirenone) and the reference preparation drospirenone ethinyl estradiol tablets (Yasmin®) (specification: each tablet contains 0.03 mg ethinyl estradiol and 3 mg drospirenone) in healthy subjects.

Start Date07 Dec 2024

Sponsor / Collaborator

Wuhan Jissbon Sanitary Product Co. Ltd.

100 Clinical Results associated with Drospirenone/Ethinyl Estradiol

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100 Translational Medicine associated with Drospirenone/Ethinyl Estradiol

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100 Patents (Medical) associated with Drospirenone/Ethinyl Estradiol

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289

Literatures (Medical) associated with Drospirenone/Ethinyl Estradiol

01 Oct 2024·European Journal of Obstetrics & Gynecology and Reproductive Biology

Safety assessment of Yasmin: Real-world adverse event analysis using the FAERS database

Article

Author: Wang, Jiahui ; Xu, Wenting ; Zhu, Lili ; Wang, Lihong ; Tang, Xiuqin ; Shi, Lingli ; Chen, Qingli

BACKGROUNDThis study aimed to elucidate the scope and nature of adverse events (AEs) associated with Yasmin.METHODSAmong the 17,035,572 AE reports collected from the Food and Drug Administration Adverse Event Reporting System (FAERS) database between January 2004 and September 2023, 25,949 reports involved Yasmin. The demographic details, clinical outcomes, and sources of reports were extracted, and four algorithms were used to evaluate adverse drug reactions.RESULTSThe majority of the AE reports involved females aged 18-45 years. Hospitalization was the most frequently reported serious outcome (46.84 %), with death occurring in 292 patients (1.82 %). The highest number of reports originated from the United States. Adverse reactions spanned across 24 system organ categories (SOCs), and hepatobiliary, vascular, and psychiatric disorders were the most frequently reported AEs. A total of 229 Preferred Terms (PTs) were identified for adverse reactions, with high signal strength observed for conditions such as post-cholecystectomy syndrome. In addition, fear of disease, which has not been previously identified as an AE related to Yasmin, was also identified as a high signal strength side effect.CONCLUSIONThe findings of the present study underscore the importance of monitoring and identifying potential AEs in patients receiving Yasmin, including those not currently listed in the medication instructions.

04 Jul 2023·Acta Clinica Belgica

Inconsistencies in laboratory investigations of hypertension in a young woman taking ethinylestradiol/drospirenone association

Article

Author: Cavalier, Etienne ; Dufour, Patrice ; Le Goff, Caroline ; Vroonen, Laurent

CASE PRESENTATIONA 34-year-old woman presented to the emergency department for arterial hypertension. Blood analysis requested by the endocrinologist showed very high level of aldosterone (1805 ng/L, normal values: <264 ng/L) and high level of renin activity (2.8 ng/mL/h, normal values: 0.1-2.0 ng/mL/h). The patient reported the use of Yasmin® (ethinylestradiol 30 µg/drospirenone 3 mg) continuously (without hormone-free week between cycles) as oral contraception. Medical imaging examinations revealed no anomaly in the kidneys and the adrenal glands. On the endocrinologist advice, patient stopped the intake of Yasmin®. Aldosterone and renin levels were measured several times after the discontinuation of the oral contraception and a diminution of these levels was observed with a complete normalization of both levels 26 days after the synthetic hormones discontinuation.DISCUSSIONThe literature shows that ethynilestradiol/drospirenone association can interfere with the renin-angiotensin-aldosterone system and increase the levels of aldosterone and/or renin. We reported here a clinical case illustrating the significant impact of this medication on the renin-angiotensin-aldosterone axis of a young woman. However, this association is not listed among the drugs interfering with the aldosterone and renin-level measurements.CONCLUSIONConsidering the data in the literature and our clinical case, we suggest adding drospirenone and the ethinylestradiol/drospirenone association in the list of drugs interfering with aldosterone and renin level determination.

03 Aug 2022·Gynecological Endocrinology

Effect of orlistat during individualized comprehensive life-style intervention on visceral fat in overweight or obese PCOS patients

Article

Author: Ruan, Xiangyan ; Mueck, Alfred Otto ; Xu, Zhongting ; Luo, Suiyu ; Min, Min ; Li, Meng ; Cheng, Jiaojiao ; Wang, Husheng

ObjectiveTo investigate the effect of orlistat combined with drospirenone/ethinylestradiol tablets (DRSP/EE) on the visceral fat area (VFA) compared to DRSP/EE-alone in overweight or obese patients with polycystic ovary syndrome (PCOS).Methods90 PCOS patients [body mass index (BMI) ≥24kg/m²] were recruited for a prospective, open-label, 1:2 paired 3-monthly study. All were included during the per-protocol defined recruitment time and numbered according to the entry-order: group-1: No.1-60, orlistat plus DRSP/EE; group-2: No.61-90, DRSP/EE-alone. Both groups received the same comprehensive intervention in terms of individualized, standardized management and lifestyle monitoring such as diet and exercise. Primary study-endpoint was VFA, secondary endpoints were anthropometric indices, sex hormones and glucolipid metabolism. Within- and between-group analyses were performed.ResultsVFA [cm²] in group-1 after treatment decreased significantly (p = 0.001), and the between-group comparison was highly significant (p = 0.001). Body weight, hip circumference (HC), BMI, body fat (BF), free testosterone (FT) and low-density lipoprotein-cholesterol (LDL-C) significantly decreased in both groups (within-group analysis); the decrease in group-1 was significantly greater than in group-2 (p < 0.05). Systolic and diastolic blood pressure (SBP/DBP) and fasting plasma glucose (FPG) in group-1 were significantly decreased, significantly more in group-1 than in group-2 (p < 0.05).ConclusionThis study is the first to investigate the effect of orlistat combined with DRSP/EE in overweight or obese PCOS patients compared with using DRSP/EE-alone. Orlistat combined with DRSP/EE was better than using DRSP/EE-alone in reducing VFA, body weight, FT, BP and FPG, which provides evidence for the choice of rational drug use in clinical practice.

1

News (Medical) associated with Drospirenone/Ethinyl Estradiol

27 Oct 2009

·www.pharmatimes.com

Bayer earnings fall again but pharma sales are healthy

Bayer has posted a decline in earnings and sales for the third quarter this morning, but pharmaceuticals continued to perform well as the German firm’s CropScience unit dragged the figures down. Net income fell 10.1% to 249 million euros, a less dramatic decline than expected by analysts, while group turnover was down 7.0% to 7.39 billion euros. However, sales at Bayer’s healthcare division were up 3.5% to 3.94 billion euros, helped by a favourable currency impact, while pharmaceutical revenues increased 3.0% to 2.55 billion euros. Growth was driven by Betaferon/Betaseron (interferon beta 1b) for multiple sclerosis (283 million euros; -2.7%) and the Yasmin (ethinyl estradiol/drospirenone) contraceptive franchise which climbed 3.9% to 320 million euros. Mirena, the firm’s levonorgestrel-releasing intrauterine contraceptive system, contributed 105 million euros, flat on the like, year-earlier period. The haemophilia agent Kogenate (recombinant antihaemophilic factor), edged up 5.1% to 247 million euros, while Nexavar (sorafenib), which is approved for liver as well as advanced kidney cancer, contributed 161 million euros, up 33.1%. Sales of the hypertension treatment Adalat (nifedipine) were up 4.7% to 155 million euros and the erectile dysfunction drug Levitra (vardenafil) climbed 12.2% to 92 million euros. As for Bayer’s antibiotics, Cipro/Ciprobay (ciprofloxacin) brought in 83 million euros, down 1.2%, while Avelox (moxifloxacin) fell 8.9% to 92 million euros. Chairman Werner Wenning said the group achieved a slight year-on-year increase in underlying profits for the first time this year and said “we are very pleased to have reversed the earnings trend despite the fact that many industries are still suffering from the economic crisis”. He added that Bayer is “still adhering to our ambitious full-year forecast” of 31- 32 billion euros in sales and limiting the decline in earnings before interest, taxes, depreciation and amortisation and special items, to 5%. The company plans to complete its current restructuring programmes by the end of 2009, and estimates the special charges involved in that process will reach 350 million euros, up from a previous estimate of 250 million euros.

100 Deals associated with Drospirenone/Ethinyl Estradiol

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Dysmenorrhea	Japan	Bayer AG	15 May 2019
Endometriosis	Japan	Bayer AG	19 Dec 2016
Premenstrual Dysphoric Disorder	United States	Bayer HealthCare	04 Oct 2006
Contraception	Netherlands	Bayer BV	08 Aug 2000

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Contraception	Phase 1	Austria	Bayer AG	01 Mar 2004
Contraception	Phase 1	Finland	Bayer AG	01 Mar 2004
Contraception	Phase 1	Lithuania	Bayer AG	01 Mar 2004
Contraception	Phase 1	Estonia	Bayer AG	01 Mar 2004
Primary dysmenorrhea	Discovery	Germany	Bayer AG	01 Dec 2007
Primary dysmenorrhea	Discovery	United Kingdom	Bayer AG	01 Dec 2007
Contraception	Discovery	Estonia	Bayer AG	01 Mar 2004
Contraception	Discovery	Austria	Bayer AG	01 Mar 2004
Contraception	Discovery	Lithuania	Bayer AG	01 Mar 2004
Contraception	Discovery	Finland	Bayer AG	01 Mar 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00567164 (CTgov)	Phase 3	Contraception	1,887	EE20/DRSP (BAY86-5300) (Flexible (Extended) Regimen no. 1 of EE20/DRSP (BAY86-5300))	xrpcnrixay(prwukvuclx) = oqudcehudk whyefnarkr (lvcxektura, fnivdakrym - hrgyfhhheh) View more	-	12 Mar 2014
				EE20/DRSP (BAY86-5300) (Flexible (Extended) Regimen no. 2 of EE20/DRSP (BAY86-5300))	sioaqikqjr(regpsvcags) = vxlmozlbfe mlndbbzbbf (uyzatkwnpi, eodsvezocj - izocsiipki) View more
NCT01258660 (CTgov)	Phase 1	Contraception	172	folic acid placebo+EE 0.03 mg/DRSP 3 mg (Yasmin) (EE 0.03 mg/DRSP 3 mg/Metafolin + Folic Acid Placebo)	yxucujtxbo(jfmiszisbw) = urnxsuarak gzgvhgifaz (apstnvhjln, sgmgcjoqif - vbfvhqglaz) View more	-	13 May 2011
				folic acid+EE 0.03 mg/DRSP 3 mg (Yasmin) (EE 0.03 mg/DRSP 3 mg (Yasmin) + Folic Acid)	yxucujtxbo(jfmiszisbw) = jgtnuqoown gzgvhgifaz (apstnvhjln, vnepirxcva - fuwcnuqxws) View more
NCT01182207 (CTgov)	Phase 1	-	33	Ethinyl Estradiol+Drospirenone (Drospirenone/Ethinyl Estradiol (Test))	xcxtzceqsl(tzmbjslycl) = glxokpeseh lcdqixrotq (ryrulowdmy, lhufandrtl - bcsravfnxt) View more	-	07 Oct 2010
				YAZ (YAZ® (Reference))	xcxtzceqsl(tzmbjslycl) = vmyxbfjaxf lcdqixrotq (ryrulowdmy, jvxstqutbp - lolpgrywkd) View more
NCT01182194 (CTgov)	Phase 1	-	32	Ethinyl Estradiol+Drospirenone (Drospirenone/Ethinyl Estradiol (Test))	obxaguywvp(ulvciqkuqn) = kpprcetptl crgteiilgi (ypykhpcrks, ptsnorlgpn - romejesdsi) View more	-	07 Oct 2010
				YAZ (YAZ® (Reference))	obxaguywvp(ulvciqkuqn) = ubtahmqzkd crgteiilgi (ypykhpcrks, ylovlaqwsr - hfqgraqwop) View more
NCT00511797 (CTgov)	Phase 2/3	Dysmenorrhea	249	SH T04740B (DRSP 1 mg/EE 20 μg)	oojtycahkd(fdkvktpogm) = obzccbbvlq geycomirxp (grldfxnavu, rzpvvjctms - lgfczubhks) View more	-	04 Oct 2010
				SH T04740F (DRSP 2 mg/EE 20 μg)	oojtycahkd(fdkvktpogm) = utotiwysgv geycomirxp (grldfxnavu, laftqamfmd - shryqfsott) View more
NCT00266032 (CTgov)	Phase 3	Contraception	1,166	Flexible (extended) treatment of EE20/DRSP (YAZ, BAY86-5300) (Flexible (Extended) Treatment of EE20/DRSP (YAZ, BAY86-5300))	ncozfkcuch(yxerevqipz) = hiaiiayonn tlsbjiiuxn (xzyshizutt, bgbocqtykr - eurmrzkjoe) View more	-	03 Mar 2010
				Fixed extended treatment of EE20/DRSP (YAZ, BAY86-5300) (Fixed Extended Treatment of EE20/DRSP (YAZ, BAY86-5300))	ncozfkcuch(yxerevqipz) = ytrbhjwttn tlsbjiiuxn (xzyshizutt, gfsvcpypgx - pyonmmpgom) View more