Delving into the Latest Updates on Dienogest/Estradiol Valerate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

ESTRADIOL VALERATE/ESTRADIOL VALERATE/DIENOGEST, BAY86-5027, SH T00658K

+ [4]

Target

ER x PR

Action

agonists

Mechanism

ERs agonists(Estrogen receptors agonists), PR agonists(Progesterone receptor agonists)

Therapeutic Areas

Endocrinology and Metabolic DiseaseUrogenital DiseasesOther Diseases+ [1]

Active Indication

MenorrhagiaContraceptionOestrogen deficiency+ [1]

Inactive Indication

Female sexual dysfunctionHeadacheMetrorrhagia

Originator Organization

Bayer AG

Active Organization

Bayer HealthCare AG

Bayer HealthCare Pharmaceuticals, Inc.Bayer BV

+ [2]

Inactive Organization

Bayer AG

Drug Highest PhaseApproved

First Approval Date

Spain (08 May 2001),

Oestrogen deficiency

Regulation-

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Structure/Sequence

Molecular FormulaC43H57NO5

InChIKeyLRHSUZNWLAJWRT-GAJBHWORSA-N

CAS Registry307334-58-3

The goal of this clinical trial is to learn if Estetrol/Drospirenone inhibit ovulation in quick-starting method. It will also learn about the safety of Estetrol/Drospirenone. The main questions it aims to answer are:
Does Estradiol valerate/Dienogest inhibit ovulation inferior to Ethinyl estradiol/Gestodene when starting on Day 7-9 of menstrual cycle? What are the impacts of Estradiol valerate/Dienogest on ovarian activities when starting on Day 7-9 of menstrual cycle? How does the cervical mucus change when starting Estradiol valerate/Dienogest on Day 7-9 of menstrual cycle? What are the adverse effects when starting Estradiol valerate/Dienogest on Day 7-9 of menstrual cycle? Researchers will compare Estradiol valerate/Dienogest to Ethinyl estradiol/Gestodene to see if Estradiol valerate/Dienogest inhibit ovulation in quick-starting method.

Start Date01 May 2024

Sponsor / Collaborator

University of Chulalongkorn

NCT05332106

/ CompletedPhase 1

Bioavailability of a Formulation of Estradiol Valerate and Dienogest 2 mg/2 mg Coated Tablets With Regards to the Marketed Reference Product

This study will investigate the bioavailability in fasting healthy, adult, human post-menopausal female subjects of 1 tablet formulation containing Estradiol Valerate and Dienogest 2 mg/ 2mg.
The study will be performed at a single site with 10 subjects. Participants will take 1 tablet of the test product and reference product in 2 periods and 2 sequences (either test after reference or reference after test). There will be a washout of at least 7 days between each study period.

Start Date12 Mar 2022

Sponsor / Collaborator

Laboratorios Andrómaco SA

100 Clinical Results associated with Dienogest/Estradiol Valerate

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100 Translational Medicine associated with Dienogest/Estradiol Valerate

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100 Patents (Medical) associated with Dienogest/Estradiol Valerate

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59

Literatures (Medical) associated with Dienogest/Estradiol Valerate

01 Oct 2016·ContraceptionQ2 · MEDICINE

Bleeding pattern and cycle control with estetrol-containing combined oral contraceptives: results from a phase II, randomised, dose-finding study (FIESTA)

Q2 · MEDICINE

Article

Author: Mawet, Marie ; Coelingh Bennink, Herjan J T ; Maillard, Catherine ; Zimmerman, Yvette ; Apter, Dan ; Foidart, Jean-Michel ; Beekman, Louise

OBJECTIVES:

This study aims to assess vaginal bleeding patterns and cycle control of oral contraceptives containing estetrol (E4) combined with either drospirenone (DRSP) or levonorgestrel (LNG).

STUDY DESIGN:

An open-label, multicentre, randomised, dose-finding study lasting six cycles in healthy women aged 18-35 years was used. Four treatments (15 mg or 20 mg E4, combined with either 3 mg DRSP or 150 mcg LNG) were administered in a 24/4-day regimen. A marketed dosing regimen of estradiol valerate with dienogest (E2V/DNG) served as reference since it contains (like E4) a natural oestrogen.

RESULTS:

A total of 396 women were randomised, of whom 389 received study medication, and 316 completed the study. By cycle 6, the frequencies of unscheduled bleeding and/or spotting and absence of withdrawal bleeding were the lowest in the 15 mg E4/DRSP group (33.8% and 3.5%, respectively). In the E2V/DNG reference group, these frequencies were 47.8% and 27.1%, respectively. By cycle 6, the frequency of women with absence of withdrawal bleeding was <20% for all E4 treatment groups: 3.5-3.8% combined with DRSP and 14.0-18.5% combined with LNG. By cycle 6, unscheduled intracyclic bleeding was reported by <20% of women in the 20 mg E4/LNG group (18.9%) and in the 15 mg E4/DRSP group (16.9%).

CONCLUSION:

This study showed that, of the four treatment modalities investigated, the 15 mg E4/DRSP combination has the most favourable bleeding pattern and cycle control.

IMPLICATIONS:

Due to its favourable bleeding pattern and cycle control, the 15 mg E4/DRSP combination is the preferred combination for further phase III clinical development.

01 Oct 2015·Archives of gynecology and obstetricsQ4 · MEDICINE

Are hormonal components of oral contraceptives associated with impaired female sexual function? A questionnaire-based online survey of medical students in Germany, Austria, and Switzerland

Q4 · MEDICINE

Article

Author: Florin-Andrei Taran ; Birgitt Schönfisch ; Christian W. Wallwiener ; Harald Seeger ; Sara Y. Brucker ; Markus Wallwiener ; Stephan Zipfel ; Alfred O. Mueck ; Lisa-Maria Wallwiener ; Johannes Bitzer

PURPOSE:

To investigate in a large cohort of young university women whether different progestins and different ethinyl estradiol (EE) dosages in oral hormonal contraceptives (OHCs) adversely affect sexual function.

METHODS:

Female medical students from German, Austrian, and Swiss universities (14/1/1) completed an anonymous online questionnaire comprising the 19 Female Sexual Function Index (FSFI) questions and 17 additional questions concerning demographics, lifestyle, sexual activity, and contraceptive use. OHCs were categorized by EE dose (≤20, <20 to ≤30, and >30 µg) and partially androgenic or antiandrogenic progestins. FSFI scores were analyzed by contraceptive method using descriptive statistics and standard nonparametric tests.

RESULTS:

We analyzed 2612 questionnaires submitted by respondents aged ≤30 years [mean age (SD) 23.5 (2.5) years]. Of 2126 contraceptive users, 1535 (72.2 %) used OHCs. Median FSFI total scores (ranges) were 28.2 (2.0-36.0) for all respondents. Median FSFI was significantly lower in non-users (24.4) versus users (28.7) of contraception (p < 0.001). Stratified analysis showed that 279/486 (57.4 %) respondents using no contraceptives, 563/1535 (36.7 %) using OHCs, 71/227 (31.3 %) using non-oral hormonal contraceptives, and 96/351 (27.4 %) using non-hormonal contraceptives were at risk for female sexual dysfunction (FSFI total score <26.55). FSFI scores for the three EE dosage categories and progestin components did not differ significantly.

CONCLUSIONS:

For OHCs, the FSFI score was lower than for other contraceptives but there was no significant association with EE dose or progestins, possibly due to small sample sizes. Further research needs to clarify the role of OHCs in female sexual function.

01 Jul 2015·Gynecological endocrinology : the official journal of the International Society of Gynecological EndocrinologyQ4 · MEDICINE

Effectiveness, tolerability and acceptance of a low-dosed estradiol/dienogest formulation (Lafamme 1 mg/2 mg) for the treatment of menopausal complaints: a non-interventional observational study over 6 cycles of 28 days.

Q4 · MEDICINE

Article

Author: Daniela Rouskova ; Katrin Mittmann ; Thomas Zimmermann ; Ulrike Schumacher ; Horst Dietrich

BACKGROUND:

Concern and controversy characterize nowadays the use of hormone therapy for management of patients with menopausal complaints. This observational non-interventional study examined the use of a marketed oral formulation containing 1 mg estradiol valerate and 2 mg dienogest for treatment of menopausal symptoms in 1292 women visiting 243 gynecological practices in Germany.

METHODS:

Score changes in the Menopausal Rating Scale (MRS) after three and six 28-day cycles were primary endpoints. Subjective reports on skin- and hair-related complaints and satisfaction with treatment effects were assessed. The incidence of adverse drug reactions (ADRs), adverse events (AEs) and vaginal bleeding was evaluated.

RESULTS:

MRS total score decreased substantially and stronger than the clinically relevant change of 5 points (p < 0.0001) as compared with baseline. Subjective skin- and hair-related complaints declined. No unexpected ADRs were reported. AEs (including ADRs) were registered in 8.8% of the participants; most frequent AEs/ADRs were postmenopausal hemorrhage (2.9%) and drug ineffective (1.4%). Nearly 76% of the subjects remained amenorrheic. Approximately 90% of the patients rated the medication's effectiveness/tolerability as good/very good; 84% intended to continue the treatment.

CONCLUSION:

This low-dose estradiol/dienogest formulation proved efficient and well-tolerated option for the alleviation of menopausal symptoms associated with estrogen deficiency.

100 Deals associated with Dienogest/Estradiol Valerate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	G03AB08	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Menorrhagia	United States	Bayer HealthCare Pharmaceuticals, Inc.	14 Mar 2012
Contraception	Australia	Bayer Australia Ltd.	14 May 2009
Oestrogen deficiency	Netherlands	Bayer BV	08 May 2001
Oestrogen deficiency	Portugal	Bayer BV	08 May 2001
Oestrogen deficiency	Spain	Bayer BV	08 May 2001

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Metrorrhagia	Phase 3	China	Bayer AG	01 Jun 2012
Metrorrhagia	Phase 3	Philippines	Bayer AG	01 Jun 2012
Metrorrhagia	Phase 3	Russia	Bayer AG	01 Jun 2012
Metrorrhagia	Phase 3	Singapore	Bayer AG	01 Jun 2012
Metrorrhagia	Phase 3	Taiwan Province	Bayer AG	01 Jun 2012
Metrorrhagia	Phase 3	Thailand	Bayer AG	01 Jun 2012
Primary dysmenorrhea	Phase 3	United States	Bayer AG	01 Apr 2009
Primary dysmenorrhea	Phase 3	Canada	Bayer AG	01 Apr 2009
Primary dysmenorrhea	Phase 3	Chile	Bayer AG	01 Apr 2009
Primary dysmenorrhea	Phase 3	Italy	Bayer AG	01 Apr 2009

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02352090 (SYLVI, CTgov)	Phase 4	Inflammation \| Contraception	59	Ethinyl estradiol / dienogest (Synthetic Estrogen + Progestin)	lwvdjdvxtg(fmnrdrimbc) = totstwkiwl vuupqcddfe (ftzzqprigl, zutghdmkrb - ugyrmvdnbw) View more	-	29 Jun 2021
				Estradiol valerate / dienogest (Natural Estrogen + Progestin)	lwvdjdvxtg(fmnrdrimbc) = umpeorrbgq vuupqcddfe (ftzzqprigl, ihtbzrwkaf - perogtsbac) View more
NCT01638910 (Pubmed \| Int J Womens Health)	Phase 3	-	954	Estradiol valerate/dienogest	tdjxjintxz(nhumvjwhwc) = tetujntddz tqrqauxagc (mikvypatxo )	-	01 Jan 2018
NCT00754065 (CTgov)	Phase 3	Contraception	409	Estradiol valerate, Dienogest (Natazia, Qlaira, BAY86-5027) (Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027))	uxewehidsp(ojiedjzrkv) = nlsfuhhtwo wcgnijdnzi (xlakgsysab, 23.58) View more	-	28 Aug 2012
				Ortho Tri Cyclen Lo (Ortho Tri-Cyclen Lo)	uxewehidsp(ojiedjzrkv) = ttssenwqld wcgnijdnzi (xlakgsysab, 25.90) View more
NCT00764881 (CTgov)	Phase 3	Female sexual dysfunction \| Contraception	217	EV/DNG (Qlaira, BAY86-5027, SH T00658ID) (EV/DNG (Natazia, Qlaira, BAY86-5027, SH T00658ID))	wbhjdfqxpv(qkkijlhluz) = wntunilzuh leqgxadkvj (xznrvroxcs, 5.33) View more	-	03 Apr 2012
				Placebo+Microgynon (EE/LNG (Microgynon) + Placebo)	wbhjdfqxpv(qkkijlhluz) = loqsitjkte leqgxadkvj (xznrvroxcs, 6.22) View more
NCT00909857 (CTgov)	Phase 3	Primary dysmenorrhea	507	Placebo Match to SH T00658ID+Estradiol valerate, Dienogest (Natazia, Qlaira, BAY86-5027) (Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027))	ifslalzjtn(aydopykmsf) = fizqumiemr idsioxfyzl (eebvuhxnge, 4.6) View more	-	27 Feb 2012
				Placebo Match to SH D593B+Ethinyl estradiol, Levonorgestrel (Miranova) (Ethinyl Estradiol, Levonorgestrel (Miranova))	ifslalzjtn(aydopykmsf) = jrbzicoedo idsioxfyzl (eebvuhxnge, 4.2) View more
NCT00185224 (Pubmed \| Clin Drug Investig)	Phase 2	-	58	Estradiol valerate/dienogest	xbqjkositl(hbtshjhvfq) = yxvsuzjkrq hpkfmfmgsm (modsahgcnb ) View more	-	01 Jan 2011
				Ethinylestradiol/levonorgestrel	xbqjkositl(hbtshjhvfq) = yjjqgwqdfw hpkfmfmgsm (modsahgcnb ) View more
NCT00185367 (Pubmed \| Contraception)	Phase 3	Contraception	798	Estradiol valerate/dienogest	letwimgcdy(lokwbwpexu) = cgedhcznlt jhvdridbuw (gugrdehedb ) View more	-	01 Nov 2009
				Ethinyl estradiol/levonorgestrel	letwimgcdy(lokwbwpexu) = vxcxlyxnen jhvdridbuw (gugrdehedb ) View more