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, BAY-86-513

+ [20]

Target

AR x ER x MR x PR

Mechanism

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

Therapeutic Areas

Nervous System DiseasesUrogenital DiseasesOther Diseases

Active Indication

DysmenorrheaEndometriosisPremenstrual Dysphoric Disorder+ [1]

Inactive Indication-

Originator Organization

Bayer AG

Active Organization

Bayer HealthCare Pharmaceuticals, Inc.

Bayer AGBayer HealthCare

Inactive Organization

Bayer Healthcare Co., Ltd.

Bayer HealthCare AG

Bayer Pharma AG

+ [1]

Drug Highest PhaseApproved

First Approval Date

US (11 May 2001),

Contraception

Regulation-

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Structure

Molecular FormulaC44H54O5

InChIKeyJLQFVGYYVXALAG-CFEVTAHFSA-N

CAS Registry164017-31-6

The study is to compare the rate and extent of absorption of a generic formulation with that of a reference for mulation when given as equal labeled dose. The study will be randomized, open-label, single dose, two way crossover design with two-period, two-treatment and two-sequence under fasting condition and at least 28 days washout period between the doses.

Start Date05 Mar 2024

Sponsor / Collaborator

Bio-innova Co., Ltd

CTR20240529 / Active, not recruitingNot Applicable

屈螺酮炔雌醇片在空腹及餐后条件下的人体生物等效性试验

[Translation] Bioequivalence study of drospirenone and ethinyl estradiol tablets in humans under fasting and fed conditions

本研究考察健康女性受试者在空腹及餐后条件下，单次口服由广州朗圣药业有限公司提供的屈螺酮炔雌醇片（受试制剂，规格：3mg/0.03mg）与相同条件下单次口服由Jenapharm GmbH & Co. KG持证的屈螺酮炔雌醇片（参比制剂，商品名：Yasmin®，规格：3mg/0.03mg）的药动学特征，评价两制剂间的生物等效性及安全性，为该受试制剂的注册申请提供依据。

[Translation]

This study investigated the pharmacokinetic characteristics of drospirenone ethinyl estradiol tablets (test preparation, specification: 3mg/0.03mg) provided by Guangzhou Langsheng Pharmaceutical Co., Ltd. and drospirenone ethinyl estradiol tablets (reference preparation, trade name: Yasmin®, specification: 3mg/0.03mg) certified by Jenapharm GmbH & Co. KG in healthy female subjects under fasting and postprandial conditions, and evaluated the bioequivalence and safety of the two preparations to provide a basis for the registration application of the test preparation.

Start Date27 Feb 2024

Sponsor / Collaborator

Regenex Corp.

NCT06233071 / RecruitingPhase 1

A Bioequivalence Study of Drospirenone (3 mg) + Ethinyl Estradiol (0.02 mg) Tablets Relative to Yaz® in Healthy Thai Female Volunteers Under Fasting Condition

The study is to compare the rate and extent of absorption of a generic formulation with that of a reference for mulation when given as equal labeled dose. The study will be randomized, open-label, single dose, two way crossover design with two-period, two-treatment and two-sequence under fasting condition and at least 28 days washout period between the doses.

Start Date13 Feb 2024

Sponsor / Collaborator

Bio-innova 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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111

Literatures (Medical) associated with Drospirenone/Ethinyl Estradiol

04 Jul 2023·Acta clinica Belgica

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

Article

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

CASE PRESENTATION:

A 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.

DISCUSSION:

The 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.

CONCLUSION:

Considering 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.

01 Dec 2021·European journal of obstetrics, gynecology, and reproductive biologyQ4 · MEDICINE

Efficacy of dienogest vs combined oral contraceptive on pain associated with endometriosis: Randomized clinical trial

Q4 · MEDICINE

Article

Author: Lina El Taha ; Dalia Khalifeh ; Antoine Abu Musa ; Joseph Nassif ; Sehrish Abbasi ; Ali Khalil

OBJECTIVE:

To compare the efficacy of dienogest with the combined oral contraceptive pill (COC) Yasmin for the control of endometriosis-associated pelvic pain.

STUDY DESIGN:

Seventy women with endometriosis-associated chronic pelvic pain, dysmenorrhoea or both for >6 months were randomized to either dienogest (Visanne) 2 mg/day or monophasic COC (Yasmin, 0.03 mg ethinyl estradiol and 3 mg drospirenone) for 24 weeks. The primary efficacy variable was change in non-cyclic pelvic pain and dysmenorrhoea from baseline to end of treatment, assessed using a visual analogue scale (VAS). The secondary efficacy variable was change in the Biberoglu and Behrman (B&B) scale scores for chronic pelvic pain, dysmenorrhoea and dyspareunia. Health-related quality of life (HRQoL) was evaluated using the Endometriosis Health Profile-30 (EHP-30) questionnaire at baseline and 24 weeks. Safety variables included incidence of side-effects, bleeding pattern and treatment tolerability.

RESULTS:

Both treatments improved the mean VAS score for endometriosis-associated pelvic pain significantly: mean difference 6.0 [95% confidence interval (CI) 4.9-7.1; p < 0.0001] in the dienogest group and 4.54 (95% CI 3.1-5.9; p < 0.0001) in the COC group; the difference between them was not significant (p = 0.111). Similarly, both dienogest and COC improved HRQoL in various core and modular segments of the EHP-30 questionnaire with comparable requirements for supplemental pain medication (p = 0.782 and 0.258 at 12 and 24 weeks, respectively), and redistribution of the B&B severity profile for chronic pelvic pain (p = 0.052 and 0.526 at 12 and 24 weeks, respectively), dysmenorrhoea (p = 0.521 and 1 at 12 and 24 weeks, respectively) and dyspareunia (p = 0.376 and 0.835, respectively). Nevertheless, dienogest was associated with fewer side-effects, and hence had a better safety and tolerability profile than COC.

CONCLUSIONS:

Dienogest (2 mg/day) is comparable to the COC Yasmin for the relief of endometriosis-associated pelvic pain and improvement in HRQoL.

CLINICAL TRIAL REGISTRATION:

Clinicaltrials.gov under number NCT04256200; date of registration 15/1/2020 (registered retrospectively).

01 Mar 2021·The journal of obstetrics and gynaecology researchQ4 · MEDICINE

Ketogenic diet in women with polycystic ovary syndrome and liver dysfunction who are obese: A randomized, open‐label, parallel‐group, controlled pilot trial

Q4 · MEDICINE

Article

Author: Li, Fu‐Ying ; Gu, Bei ; Bai, Wen‐Pei ; Li, Jian ; Bai, Le‐Ran ; Huang, Bin ; Yan, Shu‐Xiang ; Jiang, Bo

Abstract:

Aim:

To evaluate the effect of a ketogenic diet (KD) in women with polycystic ovary syndrome (PCOS) and liver dysfunction who were obese.

Methods:

Women with PCOS and liver dysfunction who were obese were enrolled in this prospective, open‐label, parallel‐group, controlled pilot trial, and randomly received KD (KD group) or conventional pharmacological treatment (Essentiale plus Yasmin, control group) in a 1:1 ratio for 12 weeks. The primary endpoint was the liver function markers. Secondary endpoints included the menstrual cycle, anthropometric characteristics, body composition, hormonal levels, and metabolic biomarkers.

Results:

Of the 20 eligible participants enrolled, 18 participants completed the study. The KD group reported a significant reduction in anthropometric characteristics and body composition from baseline to week 12 (all p < 0.05). In addition, there were significant reductions in menstrual cycle, plasma estradiol, and progesterone levels in two groups (all p < 0.05), but no significant between‐group difference was observed. KD significantly reduced the liver function markers compared with control group (p < 0.05). The signs of fatty liver disappeared in six out of seven fatty liver participants in KD group after 12 weeks of intervention, while only one of 10 fatty liver participants in control group disappeared.

Conclusions:

In addition to improving the menstrual cycle, KD had the additional benefits of reducing blood glucose and body weight, improving liver function, and treating fatty liver compared to traditional pharmacological treatment in women with PCOS and liver dysfunction who were obese.

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
-	-	G03FA17	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Dysmenorrhea	JP	Bayer AG	15 May 2019
Endometriosis	JP	Bayer AG	19 Dec 2016
Premenstrual Dysphoric Disorder	US	Bayer HealthCare	04 Oct 2006
Contraception	US	Bayer HealthCare Pharmaceuticals, Inc.	11 May 2001

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Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02710708 \| CTR20160203 (Pubmed \| Adv Ther)	Phase 4	-	1,921	YAZ (3 mg drospirenone/20 μg ethinyl estradiol)	lymeeulzoz(ajxfvreosx) = fshsvrtaus anmbxkrncn (gvlulhpzii )	-	01 Feb 2020
International Active Surveillance Study of Women Taking Oral Contraceptives (Pubmed \| Contraception)	Not Applicable	Cardiovascular Diseases	-	DRSP24d	gabnjifjvo(dpqoyepqkv) = jbcmhnrauq qhfnqszwym (exniyhggld )	-	01 Apr 2014
				DRSP21d	gabnjifjvo(dpqoyepqkv) = narhnnvtmx qhfnqszwym (exniyhggld )
NCT00567164 (CTgov)	Phase 3	Contraception	1,887	EE20/DRSP (BAY86-5300) (Flexible (Extended) Regimen no. 1 of EE20/DRSP (BAY86-5300))	bmhvkhbsum(rdvrlfhngq) = zbdxdtxprl acpvcyzehi (hanwbfrkuj, srawyxdbdy - psptpritpm) View more	-	12 Mar 2014
				EE20/DRSP (BAY86-5300) (Flexible (Extended) Regimen no. 2 of EE20/DRSP (BAY86-5300))	niccibopzi(vwearyqzbt) = ztgonddtki xibwjlifwb (wsilkiayby, uopzumldql - oylkdbmjkc) View more
NCT00567164 (Pubmed \| Contraception)	Phase 3	-	1,864	Flexible(MIB) regimen	bhupjmwjfd(ovpwtkhwbd) = ojxkkddczw pxrwaouxzp (ylaqeoliyq, ±30) View more	-	01 Aug 2012
				Flexible(APC) regimen	bhupjmwjfd(ovpwtkhwbd) = boficbzjdc pxrwaouxzp (ylaqeoliyq, ±33)
NCT00283816 (CTgov)	Phase 3	Polycystic Ovary Syndrome \| Obesity	36	Metformin (Metformin)	vvcmtllnik(qbeweergqc) = qciemzxswo mpdqxycwhi (gwgudpqzjq, giwjxassaq - hloxeydnnk) View more	-	13 Jul 2011
				placebo (Placebo)	vvcmtllnik(qbeweergqc) = gayyshhydx mpdqxycwhi (gwgudpqzjq, opfkqdlmcv - bxuqleidii) 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)	arxwnevxfp(zhuvnjgtdb) = gxibegjzuo ucmkohqvin (pbtlkjrydz, ojzjwmwofc - uxnyxzmooj) 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)	arxwnevxfp(zhuvnjgtdb) = kmqnkwmege ucmkohqvin (pbtlkjrydz, bdiiioaqad - chetgvquel) View more
NCT01182194 (CTgov)	Phase 1	-	32	Ethinyl Estradiol+Drospirenone (Drospirenone/Ethinyl Estradiol (Test))	zcelvrwmbh(eftbjgxssd) = gndtdxzmje qqrolngjhl (sarnltkodr, gwdejnshio - urgtbwveae) View more	-	07 Oct 2010
				YAZ (YAZ® (Reference))	zcelvrwmbh(eftbjgxssd) = glzocwduml qqrolngjhl (sarnltkodr, ktajblbxso - vwrrsihper) View more
NCT01182207 (CTgov)	Phase 1	-	33	Ethinyl Estradiol+Drospirenone (Drospirenone/Ethinyl Estradiol (Test))	lgfkhtqakx(lwoqkxuqvt) = uymirsxnbu oawvjpybla (opbxdlsesm, gndamonaph - fkwowtxbim) View more	-	07 Oct 2010
				YAZ (YAZ® (Reference))	lgfkhtqakx(lwoqkxuqvt) = jmldmjqgde oawvjpybla (opbxdlsesm, beigjqonmu - wuqbiwpnko) View more
NCT00511797 (CTgov)	Phase 2/3	Dysmenorrhea	249	SH T04740B (DRSP 1 mg/EE 20 μg)	gweqkgagwd(jgthpokytd) = kjrefigppl huvtiazdde (odmupcwaxa, ulvgnqlgdx - bmwiimievp) View more	-	04 Oct 2010
				SH T04740F (DRSP 2 mg/EE 20 μg)	gweqkgagwd(jgthpokytd) = jdmfbuyndr huvtiazdde (odmupcwaxa, epkfdjygnb - gcsjakjzvf) 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))	kfwrcxwqgw(pzfidenccs) = rjdcrwpmbg vnguhqozaa (xwtuznposy, cthnlcvqkz - egmkljotup) View more	-	03 Mar 2010
				Fixed extended treatment of EE20/DRSP (YAZ, BAY86-5300) (Fixed Extended Treatment of EE20/DRSP (YAZ, BAY86-5300))	kfwrcxwqgw(pzfidenccs) = hdainymiwm vnguhqozaa (xwtuznposy, jmiulxjxfx - jggycslfol) View more