Delving into the Latest Updates on Drospirenone/Estradiol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Angeliq, Angeliq low-low, Estradiol and Drospirenone

+ [8]

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

Cardiovascular DiseasesEndocrinology and Metabolic DiseaseSkin and Musculoskeletal Diseases+ [2]

Active Indication

Menopausal syndromeOsteoporosis, PostmenopausalVascular Diseases+ [3]

Inactive Indication

Essential HypertensionHypertensionPrehypertension

Originator Organization

Bayer AG

Active Organization

Searchlight Pharma, Inc.Startup

Bayer HealthCare Pharmaceuticals, Inc.Bayer Vital GmbH

Inactive Organization

Bayer AG

Drug Highest PhaseApproved

First Approval Date

United States (28 Sep 2005),

Vasomotor symptomVulvovaginal atrophy

Regulation-

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Structure/Sequence

Molecular FormulaC42H54O5

InChIKeyQJUXBIVLOGRZSQ-OQMMLGNJSA-N

CAS Registry350818-73-4

This study compares the effects of two common hormone medications on the heart and blood vessels of healthy post-menopausal women over the age of 45.
The study will take place over the course of about 5 months. Each subject will take two different medications over two six-week periods. They will be randomized at the beginning of the study to either estradiol+medroxyprogesterone acetate or estradiol+drospirenone for the first period, and will receive the other medication the second six-weeks of the study. At the very beginning of the study and at the end of each six-week treatment period, subjects will come to the hospital various tests including non-invasive blood vessel imaging tests, blood draws to test the levels of certain hormones in the body, an oral glucose tolerance test, a test to monitor renal blood flow, and 24-hour blood pressure monitoring. Between treatment periods, there will be a four-week medication-free washout period.

Start Date01 Dec 2009

Sponsor / Collaborator

The Brigham & Women's Hospital, Inc.

[+1]

NCT00785317

/ Unknown statusPhase 4IIT

Effects of Oral 1 mg Oestradiol (E2)/ 2 mg of Drospirenone (DRSP) Compared to Oral 1 mg of Oestradiol (E2)/ 0.5 mg Noresthisterone Acetate (NETA)on the Postmenopausal Breast; a Double Blind Randomized Prospective Study

The purpose of this study is to evaluate the effects on breast in postmenopausal women randomized to either oestradiol in combination with DRSP or E2 in combination with NETA during six months.

Start Date01 Nov 2008

Sponsor / Collaborator

Karolinska Institutet

100 Clinical Results associated with Drospirenone/Estradiol

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100 Translational Medicine associated with Drospirenone/Estradiol

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100 Patents (Medical) associated with Drospirenone/Estradiol

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37

Literatures (Medical) associated with Drospirenone/Estradiol

01 Jan 2018·KardiologiiaQ4 · MEDICINE

Structural and functional changes of blood vessels in women in early postmenopause, the possibility of correction of the revealed violations

Q4 · MEDICINE

Article

Author: Tolstov, S N ; Salov, I A ; Rebrov, A P

AIMTo evaluate severity and pattern of structural and functional changes of vascular wall in early postmenopausal women receiving chronic treatment with a low-dose combination of 17β-estradiol (E2) 1 mg and drospirenone 2 mg (DRSP). Evaluation of structural and functional arterial remodeling might be important for assessment of cardiovascular risk in postmenopausal women.MATERIALS AND METHODSThe study included 162 early postmenopausal women with postmenopausal syndrome. The women were divided into two groups. The main group consisted of 84 patients receiving the postmenopausal hormonal therapy (PMHT) with E2 1 mg / DRSP 2 mg (Angeliq, Bayer) and the control group included 78 women not receiving PMHT. The follow-up duration was 5.2 years. 24‑h blood pressure monitoring with evaluation of arterial stiffness (RWTT, AIx, ASI, AASI, (dP/dt) max) was performed. Endothelium-dependent dilation of the brachial artery was measured using the reactive hyperemia test. Aortic pulse wave velocity (aPWV) and common carotid intima-media thickness (ccIMT) were measured ultrasonically.RESULTSAt baseline, increased aPWV was observed in 15 (21.4 %) women of the main group and 19 (24.3 %) women of the control group (р=0.4). At the end of study, increased aPWV was observed in both groups but the increase was more pronounced in the control group. Increased pulse blood pressure (PBP) was observed in 27 (32.1 %) patients of the main group and 26 (33.3 %) patients of the control group (р=0.87). At the end of study, PBP decreased from 47.2±7.2 to 45.3±6.9 mm Hg (р.

16 Jun 2015·Zhonghua yi xue za zhi

[Clinical and metabolic effects of drospirenone-estradiol versus tibolone in postmenopausal women:a comparative study].

Article

Author: Zhang, Zhenyu ; Cheng, Jiao

OBJECTIVETo compare the clinical and metabolic effects of drospirenone-estradiol (Angeliq) versus tibolone (Livial) in postmenopausal women.METHODSTwenty-seven postmenopausal women of group 1 took Angeliq (1 dose every two days) while another group 2 (n = 26) received tibolone (2.5 mg every two days) as hormone replacement therapy for 12 weeks. A retrospective analysis was used to evaluate the clinical efficacy, safety and risk factors of cardiovascular metabolism. The clinical data were collected before and after treatment, including personal interview, medical examination and ultrasound imaging of pelvic, breast and carotid artery.RESULTSNo statistically significant inter-group differences existed in age or body mass index. Before treatment, the level of E2 was (12 ± 10) ng/L, triglyceride (TG) (2.0 ± 1.1) mmol/L, lipoprotein-a (LPa) (47 ± 43) mmol/L in group 1 versus (23 ± 12) ng/L, (1.3 ± 0.7) mmol/L and (28 ± 14) mmol/L in group 2. After 12-week treatment, (30 ± 18) ng/L, (1.6 ± 1.1) mmol/L and (37 ± 36) mmol/L in group 1 versus (23 ± 9) ng/L, (1.1 ± 0.6) mmol/L and (18 ± 12) mmol/L in group 2. A greater incidence of vaginal bleeding and thicker endometrium were found in group 1.CONCLUSIONAngeliq can relieve menopausal symptoms. And its functions of regulating lipid metabolism and protecting cardiovascular system are better than those of Livial. However, its wider acceptability is limited by vaginal bleeding, thicker endometrium and breast pain.

01 Jul 2014·MaturitasQ3 · MEDICINE

Treatment of climacteric symptoms in breast cancer patients: A retrospective study from a medication databank

Q3 · MEDICINE

Article

Author: Ameye, Lieveke ; Antoine, Caroline ; Rozenberg, Serge ; Paesmans, Marianne

INTRODUCTIONWomen affected by breast cancer (BC) will often go through menopause at an earlier age and display more frequent and severe symptoms than women who have a natural menopause. The safety of hormone replacement therapy (HRT) and vaginal estrogens for BC survivors has been debated over time and remains unclear. Non hormonal therapies such as antidepressants, gabapentine and clonidine may be useful for those patients but there are few data about their safety.AIMThis retrospective study analyses the use by BC patients of treatments known to alleviate climacteric symptoms.MATERIAL AND METHODPost-menopausal Estrogen Receptors positive (ER+) BC patients, aged 45-69, were identified as having bought, at least once, an aromatase inhibitor (AI) or tamoxifen between the years 2000 and 2012 through a pharmaceutical databank in Belgium. Among them, we defined users of a climacteric treatment those who bought, at least once, HRT, vaginal topical estrogens, antidepressants, clonidine and gabapentine.RESULTSWe identified 2530 BC patients. Among them, 45% were buying a treatment known to alleviate menopausal symptoms. The majority of these treatments were non-HRT therapies. HRT and vaginal estrogens were seldom bought (respectively 1.1% and 6%), but 3% bought vaginal estrogens while buying AI. About 9.2% of tamoxifen users patients bought antidepressants implicated in tamoxifen metabolism at the same time as tamoxifen.CONCLUSIONSMost BC patients follow current guidelines contra-indicating the use of HRT after BC, they use non hormonal therapies. In some cases they use unfortunately antidepressants that may alter the metabolism of tamoxifen.

100 Deals associated with Drospirenone/Estradiol

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Drospirenone/Estradiol	G03AA G03FA	-

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Menopausal syndrome	China	Bayer HealthCare Pharmaceuticals, Inc.	11 Jan 2015
Osteoporosis, Postmenopausal	China	Bayer Vital GmbH	29 Sep 2009
Vascular Diseases	China	Bayer Vital GmbH	29 Sep 2009
Vasomotor symptom	United States	Bayer HealthCare Pharmaceuticals, Inc.	28 Sep 2005
Vulvovaginal atrophy	United States	Bayer HealthCare Pharmaceuticals, Inc.	28 Sep 2005
Contraception	Canada	Searchlight Pharma, Inc.Startup	-

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Contraception	Phase 1	Germany	Bayer AG	01 Feb 2008
Hypertension	Phase 1	United States	Bayer AG	01 Jan 2007
Prehypertension	Phase 1	United States	Bayer AG	01 Jan 2007
Vasomotor symptom	Phase 1	South Korea	Bayer AG	01 Jul 2004
Essential Hypertension	Phase 1	-	Bayer AG	01 Apr 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00522873 (CTgov)	Phase 3	-	662	0.25mg DRSP / 0.5mg E2 (BAY86-4891) (0.25mg DRSP / 0.5mg E2 (BAY86-4891))	jqosoztnej(avjjlaebwo) = eptlggyrql aybltlantw (fsxoksjnxl, kiohmgcjrh - gpflqcvhcc) View more	-	28 Jun 2012
				0.5mg NETA / 1.0mg E2 (Activella) (0.5mg NETA / 1.0mg E2 (Activella))	kdhqozdfjb(zixogpduvj) = efffewnzky ctynpakrjd (mskbhzthvw, agaipxitms - purlwmopyc) View more
NCT00446199 (CTgov)	Phase 3	Vasomotor symptom	735	0.5mg DRSP / 0.5mg E2 (BAY86-4891) (0.5mg DRSP / 0.5mg E2 (BAY86-4891))	ovemvyzcsa(zmmpifgsjd) = tvfxvscnum yvoufbdthu (ewsvkriwiu, cnbblyitxb - hvhbqsqvxv) View more	-	18 Apr 2012
				0.25mg DRSP / 0.5mg E2 (BAY86-4891) (0.25mg DRSP / 0.5mg E2 (BAY86-4891))	ovemvyzcsa(zmmpifgsjd) = gskdamjepm yvoufbdthu (ewsvkriwiu, ttlfkgfazq - bjzuztwiny) View more
NCT00420342 (CTgov)	Phase 2	Hypertension \| Prehypertension	92	Drospirenone/17ß-estradiol (Angeliq, BAY86-4891) (0.5mg DRSP / 1.0mg E2 (Angeliq, BAY86-4891))	woxhuewffu(mvlhubxnwp) = vnacnjjfpd ifmykwagbp (ghfvwsrxag, habhkaddfr - igepoopgzf) View more	-	20 Jan 2010
				Drospirenone/17ß-estradiol (Angeliq, BAY86-4891) (2.0mg DRSP / 1.0mg E2 (Angeliq, BAY86-4891))	woxhuewffu(mvlhubxnwp) = divygynsxn ifmykwagbp (ghfvwsrxag, keilykwjib - efrjkedqzz) View more