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, Climodien, Natazia

Target

ER x PR

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 dysfunctionHeadache

Originator Organization

Bayer AG

Active Organization

Bayer HealthCare AG

Bayer HealthCare Pharmaceuticals, Inc.Bayer BV

+ [1]

Inactive Organization

Bayer AGSchering GmbH & Co. Produktions KG

Bayer Healthcare Co., Ltd.

+ [1]

Drug Highest PhaseApproved

First Approval Date

NL (08 May 2001),

Oestrogen deficiency

Regulation-

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Structure/Sequence

Molecular FormulaC20H25NO2

InChIKeyAZFLJNIPTRTECV-FUMNGEBKSA-N

CAS Registry65928-58-7

View All Structures (2)

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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14

Literatures (Medical) associated with Dienogest/Estradiol Valerate

01 Jun 2024·Journal of Assisted Reproduction and Genetics

Impact of dydrogesterone use in cycles with low progesterone levels on the day of frozen embryo transfer

Article

Author: Ferreira, Pedro ; Natário, Isabel ; Santos-Ribeiro, Samuel ; Metello, Jose ; Tomás, Claudia

PURPOSEThis study aims to evaluate whether the clinical outcomes of cycles with frozen embryo transfer (FET) in hormonal replacement treatment supplemented with dydrogesterone (DYD) following detection of low circulating levels of progesterone (P4) were comparable to the results of cycles with otherwise normal serum P4 values.METHODSExtended analyses of a retrospective cohort that included FET cycles performed between July 2019 and March 2022 after a cycle of artificial endometrial preparation using valerate-estradiol and micronized vaginal P4 (400 mg twice daily). Whenever the serum P4 value was considered low on the morning of the planned transfer, 10 mg of DYD three times a day was added as a supplement. Only single-embryo transfers of a blastocyst were considered. The primary endpoint was live birth rate.RESULTSFive-hundred thirty-five FET cycles were analyzed, of which 136 (25.4%) underwent treatment with DYD. There were 337 pregnancies (63%), 207 live births (38.6%), and 130 miscarriages (38.5%). The P4 values could be modeled by a gamma distribution, with a mean of 14.5 ng/ml and a standard deviation of 1.95 ng/ml. The variables female age on the day of FET, ethnicity, and weight were associated with a variation in the serum P4 values. There were no differences in the results between cycles with or without the indication for DYD supplementation.CONCLUSIONSLive birth rate did not vary significantly in females with low and normal serum P4 levels on the day of FET when DYD was used as rescue therapy.

01 Mar 2018·Journal of Assisted Reproduction and GeneticsQ3 · MEDICINE

Estrogen treatment in infertile women with premature ovarian insufficiency in transitional phase: a retrospective analysis

Q3 · MEDICINE

Article

Author: Sergiampietri, Claudia ; Simi, Giovanna ; Basile, Stefano ; Giannarelli, Diana ; Artini, Paolo Giovanni ; Obino, Maria Elena Rosa ; Cela, Vito ; Pinelli, Sara

PURPOSEDuring the transitional phase of premature ovarian insufficiency (POI), sporadic resumption of ovulation is possible because of fluctuation of hormonal levels but the chance of spontaneous pregnancy is low, and the main perspective of childbearing in these women is egg donation or adoption. The purpose of the study was to verify whether treatment with estrogens in POI patients in transitional phase could reduce FSH levels and to evaluate if this pre-treatment could improve reproductive outcomes of in vitro fertilization (IVF).METHODSStudy patients (26) were administered with valerate estradiol 2 mg daily adding dihydrogesterone 10 mg daily during luteal phase for 3 months before IVF. Control group (26 patients) did not receive any pre-treatment. Ovarian stimulation was conducted in both groups with the same short GnRH-antagonist protocol. Clinical and laboratory data of patients were retrospectively analyzed.RESULTSIn the study group, 4/26 POI patients became spontaneously pregnant during pre-treatment. In the remaining patients, the mean level of FSH after the pre-treatment was significantly reduced compared with baseline. Levels of circulating estradiol on the day of hCG administration were significantly higher in the study group. The total number of MII oocytes retrieved and fertilized oocytes was significantly higher in the study group, as well as the number of embryos transferred for pickup and clinical pregnancy rate.CONCLUSIONSTreatment with estrogens in infertile POI patients in transitional phase reduces circulating FSH levels, hence causing potential spontaneous conception. Moreover, in these patients, estrogen pre-treatment seems to improve IVF outcomes in a GnRH-antagonist short protocol compared to no pre-treatment.

01 Nov 2014·Gynecological EndocrinologyQ4 · MEDICINE

Effects of estroprogestins containing natural estrogen on vaginal flora

Q4 · MEDICINE

Article

Author: Francesco De Seta ; Stefano Lello ; Ester Conversano ; Stefano Restaino ; Rossella De Leo ; Gianpaolo Maso ; Rubina Banco ; Maddalena Tonon ; Giulia Barbati

Estroprogestins with "natural oestrogen" has represented a new option in terms of combined hormonal contraception. So, the aim of this study is to investigate how estroprogestins with natural estrogen may modify the vaginal niche. In literature, very few studies focused on the interaction between hormonal contraception and vaginal milieu. This is a prospective comparative study. We enrolled 60 women from January 2013 to September 2013, 30 of them were administered estradiol valerate dienogest (E2V+DNG - Klaira®) in a quadriphasic regimen, while the other 30 women were administered 17-β estradiol with nomestrol acetate (EV+NOMAC - Zoely®) in a monophasic regimen. After a baseline study of vaginal milieu at recruitment of patients (Gram stain with Nugent score, vaginal pH, vaginal wet mount for the quantification of leukocytes, Lactobacilli and/or presence of Candida), we performed the same follow-up after six months of estroprogestin therapy. Our results showed that the women treated with E2V+DNG had a trend of an improvement of vaginal health in terms of increase of lactobacillar flora and reduction of vaginal pH in place of women treated with EV+NOMAC that showed a reduction of cervical mucus. Finally, our data about the effects on vaginal flora exerted by two estroprogestin pills (EPs) containing a natural estrogen suggest slight, but interesting differences in terms of vaginal ecology. These differences could be related to the type of estrogen, type of progestin, regimen of administration and, after all, to the net balance between estrogenic and progestin component of the EPs.

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	US	Bayer HealthCare Pharmaceuticals, Inc.	14 Mar 2012
Contraception	US	Bayer HealthCare Pharmaceuticals, Inc.	06 May 2010
Oestrogen deficiency	NL	Bayer BV	08 May 2001

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Headache	Phase 1	FI	Bayer AG	01 Dec 2008
Headache	Phase 1	GB	Bayer AG	01 Dec 2008
Headache	Phase 1	AU	Bayer AG	01 Dec 2008
Headache	Phase 1	TH	Bayer AG	01 Dec 2008
Headache	Phase 1	CH	Bayer AG	01 Dec 2008
Headache	Preclinical	MX	Bayer AG	01 Dec 2008
Headache	Preclinical	ES	Bayer AG	01 Dec 2008
Contraception	Preclinical	DE	Bayer AG	01 Mar 2005
Contraception	Preclinical	FR	Bayer AG	01 Mar 2005
Contraception	Preclinical	CZ	Bayer AG	01 Mar 2005

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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)	jyugovdmxq(tlbdsrbawp) = dxnqrkqpgx xdqwxmrgvi (zblhibpjri, emjapjpyxz - mvlvudnbje) View more	-	29 Jun 2021
				Estradiol valerate / dienogest (Natural Estrogen + Progestin)	jyugovdmxq(tlbdsrbawp) = ncdshcrtfy xdqwxmrgvi (zblhibpjri, jukukxeugz - yvuqlgyuyl) View more
NCT01638910 (Pubmed \| Int J Womens Health)	Phase 3	-	954	Estradiol valerate/dienogest	rhainxyusq(bftqwydhff) = jsoojbdtbv ktxzauojcu (ualjuydbds )	-	01 Jan 2018
NCT00754065 (CTgov)	Phase 3	Contraception	409	Estradiol valerate, Dienogest (Natazia, Qlaira, BAY86-5027) (Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027))	(guzgilfosn) = eqwkyxhalu oammvogizj (cqgnreovyw, qaxadwxlqt - drqtmfrxaa) View more	-	28 Aug 2012
				Ortho Tri Cyclen Lo (Ortho Tri-Cyclen Lo)	(guzgilfosn) = xdlvijjanc oammvogizj (cqgnreovyw, zrsvhnmspc - bwqejdgelh) 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))	uanxkuvmcx(ntickklmox) = uzzbolbqah rqmilvetml (rzicbkpicz, rzbrjvarde - dftvsvzbgt) View more	-	03 Apr 2012
				Placebo+Microgynon (EE/LNG (Microgynon) + Placebo)	uanxkuvmcx(ntickklmox) = juthndhpuc rqmilvetml (rzicbkpicz, cqvxilcoqh - diuvnacndh) 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))	ldvgwsoxok(omrhnhxupt) = hztefdjtee lgrnhysgns (xgpbnqkhyq, jkxwnhxaic - gxiqybrmwo) View more	-	27 Feb 2012
				Placebo Match to SH D593B+Ethinyl estradiol, Levonorgestrel (Miranova) (Ethinyl Estradiol, Levonorgestrel (Miranova))	ldvgwsoxok(omrhnhxupt) = zisvyrgszz lgrnhysgns (xgpbnqkhyq, wyyrodfxvn - lskvshhget) View more
NCT00185224 (Pubmed \| Clin Drug Investig)	Phase 2	-	58	Estradiol valerate/dienogest	(sejjksxhct) = wcnifrippm ooqqdcioms (zomyisffxp ) View more	-	01 Jan 2011
				Ethinylestradiol/levonorgestrel	(sejjksxhct) = syycdhktdw ooqqdcioms (zomyisffxp ) View more
NCT00185367 (Pubmed \| Contraception)	Phase 3	Contraception	798	Estradiol valerate/dienogest	ypmbvwwccl(iwwdxkibsz) = wjfmlkffmf nkvtfvuzam (fogudamjkl ) View more	-	01 Nov 2009
				Ethinyl estradiol/levonorgestrel	ypmbvwwccl(iwwdxkibsz) = giogsuxccp nkvtfvuzam (fogudamjkl ) View more