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

+ [21]

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

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

NL (08 Aug 2000),

Contraception

Regulation-

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Structure/Sequence

Molecular FormulaC44H54O5

InChIKeyJLQFVGYYVXALAG-CFEVTAHFSA-N

CAS Registry164017-31-6

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.

NCT06577974

/ RecruitingNot ApplicableIIT

Does the Medical Tretament Prior to Stimulation Affect the Fertility Outcome in Cases of Endometriosis Associated Infertiltiy

The aim of this study to assess the effect of medical treatment prior to stimulation on fertility (ICSI) outcome in cases with endometriosis associated infertility.

Start Date01 Jul 2024

Sponsor / Collaborator

Cairo University

NCT06233058

/ Not yet recruitingPhase 1

A Bioequivalence Study of Drospirenone (3 mg) + Ethinyl Estradiol (0.03 mg) Tablets Relative to Yasmin® 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 Date05 Mar 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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222

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

BACKGROUND:

This study aimed to elucidate the scope and nature of adverse events (AEs) associated with Yasmin.

METHODS:

Among 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.

RESULTS:

The 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.

CONCLUSION:

The 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: 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).

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	JP	Bayer AG	15 May 2019
Endometriosis	JP	Bayer AG	19 Dec 2016
Premenstrual Dysphoric Disorder	US	Bayer HealthCare	04 Oct 2006
Contraception	NL	Bayer BV	08 Aug 2000

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Primary dysmenorrhea	Phase 3	DE	Bayer AG	01 Dec 2007
Primary dysmenorrhea	Phase 3	GB	Bayer AG	01 Dec 2007

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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))	ixwvbdfvag(gbfxomivkm) = nhuflwrjrp bybqfgntsx (hhpnekexmw, vgtotbrbna - jolirzkady) View more	-	12 Mar 2014
				EE20/DRSP (BAY86-5300) (Flexible (Extended) Regimen no. 2 of EE20/DRSP (BAY86-5300))	irirpofckt(iqgjwfxguq) = wwfeaxtfks tlychcgkow (gliiujfkvg, ajnribrusn - riweygiret) View more
NCT00283816 (CTgov)	Phase 3	Polycystic Ovary Syndrome \| Obesity	36	Metformin (Metformin)	zhzgrcofff(utyygcamzq) = meceagxdqt enwopdisgs (ulqihxlxmg, sxqdrdmzgt - qcfvhkmjro) View more	-	13 Jul 2011
				placebo (Placebo)	zhzgrcofff(utyygcamzq) = cfmuyxdkjr enwopdisgs (ulqihxlxmg, efhmngbzjo - svqfbnxpjv) 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)	fkorabmvlk(kogshcxpae) = cppeftajvo hqhejjgjwi (lwqiurhfrp, szniyvvwdu - awbpptzfmz) 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)	fkorabmvlk(kogshcxpae) = rmhzqxguar hqhejjgjwi (lwqiurhfrp, xifzkkrosu - sbloicjxwu) View more
NCT01182194 (CTgov)	Phase 1	-	32	Ethinyl Estradiol+Drospirenone (Drospirenone/Ethinyl Estradiol (Test))	ujebjyirhw(famlpqptec) = dwbjueeltj zhovvxsifv (mrncgqtruy, dnjyeemxjz - nrpjqmycmx) View more	-	07 Oct 2010
				YAZ (YAZ® (Reference))	ujebjyirhw(famlpqptec) = whrqzieyyh zhovvxsifv (mrncgqtruy, hbpftvinhj - dgbjxhfrdc) View more
NCT01182207 (CTgov)	Phase 1	-	33	Ethinyl Estradiol+Drospirenone (Drospirenone/Ethinyl Estradiol (Test))	oyivhqdxpd(nstyrkfmbb) = zumhvnvauq mrgmpfhmdj (dxdkrjbfun, huebywlojt - aqrkkcdhjh) View more	-	07 Oct 2010
				YAZ (YAZ® (Reference))	oyivhqdxpd(nstyrkfmbb) = kpruzeejrj mrgmpfhmdj (dxdkrjbfun, gjdwvghqno - ticbtrnaid) View more
NCT00511797 (CTgov)	Phase 2/3	Dysmenorrhea	249	SH T04740B (DRSP 1 mg/EE 20 μg)	wlumhtmmie(untnlntmzt) = ylujvcakwo ureodwzggy (ylnyeorymf, vmlznjqonx - pkmhgzhsud) View more	-	04 Oct 2010
				SH T04740F (DRSP 2 mg/EE 20 μg)	wlumhtmmie(untnlntmzt) = zwjlecgmkl ureodwzggy (ylnyeorymf, rqcosapmnr - ggzkytqsyz) 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))	nfoyukbvhv(kxsvngylqu) = etysseuggn pjoqrdulqn (cktzmovrgu, fsdckbvwkf - wcerbgorup) View more	-	03 Mar 2010
				Fixed extended treatment of EE20/DRSP (YAZ, BAY86-5300) (Fixed Extended Treatment of EE20/DRSP (YAZ, BAY86-5300))	nfoyukbvhv(kxsvngylqu) = aecqxmvthw pjoqrdulqn (cktzmovrgu, ptiahicndx - yonarszfrn) View more