Delving into the Latest Updates on Conjugated Estrogens/Medroxyprogesterone Acetate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Conjugated estrogens/medroxyprogesterone, Methylprogesteron/conjugated estrogens, Premarin/MPA

+ [8]

Target

ER x PR

Mechanism

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

Therapeutic Areas

Cardiovascular DiseasesEndocrinology and Metabolic DiseaseSkin and Musculoskeletal Diseases+ [1]

Active Indication

Osteoporosis, PostmenopausalVasomotor symptomVulvovaginal atrophy

Inactive Indication-

Originator Organization

Wyeth AB

Active Organization

Wyeth-Ayerst LaboratoriesWyeth Pharmaceuticals LLC

Inactive Organization

Wyeth AB

Drug Highest PhaseApproved

First Approval Date

US (17 Nov 1995),

Osteoporosis, PostmenopausalVasomotor symptomVulvovaginal atrophy

Regulation-

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Structure

Molecular FormulaC22H32O3

InChIKeyFRQMUZJSZHZSGN-HBNHAYAOSA-N

CAS Registry520-85-4

The purpose of this trial is to determine the equivalence of 3 new formulations of a Premarin®/medroxyprogesterone acetate (MPA) combination tablet to the currently marketed dosage form (Prempro® [TM]). This study will be performed in healthy postmenopausal women. Each subject will participate in the study for approximately 14 weeks, including a screening evaluation within 3 weeks before the study, and four, 6-day, 5-night inpatient periods with at least a 21-day washout interval between each dose administration.

Start Date01 Feb 2008

Sponsor / Collaborator

Wyeth AB

NCT00543634 / CompletedPhase 1

Open-Label, Single-Dose, Partially Randomized, 6-Period, 6-Treatment, Crossover Bioavailability Study of 3 Pilot Formulations of Premarin®/Medroxyprogesterone Acetate (MPA) Compared With Reference Formulations of Premarin®/MPA (PREMPRO®) and MPA Suspension (Provera®) in Healthy Postmenopausal Women

The purpose of the study is to evaluate the safety and efficacy of new tablet formulations of Premarin®/medroxyprogesterone (MPA).

Start Date01 Oct 2007

Sponsor / Collaborator

Wyeth AB

[+1]

NCT00472927 / CompletedPhase 1

An Open-Label, Single-Dose, Randomized, 4-Period, Crossover, Bioequivalence Study of Three New Formulations of Premarin 0.45mg/Medroxyprogesterone Acetate (MPA) 1.5mg Compared With a Reference Formulation of Premarin/MPA (PremproTM) 0.45mg/1.5mg in Healthy Postmenopausal Women

To evaluate three new investigational tablet formulations of the Food and Drug Administration (FDA) approved medication Prempro™, Premarin combined with medroxyprogesterone acetate (MPA).

Start Date01 May 2007

Sponsor / Collaborator

Wyeth AB

100 Clinical Results associated with Conjugated Estrogens/Medroxyprogesterone Acetate

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100 Translational Medicine associated with Conjugated Estrogens/Medroxyprogesterone Acetate

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100 Patents (Medical) associated with Conjugated Estrogens/Medroxyprogesterone Acetate

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40

Literatures (Medical) associated with Conjugated Estrogens/Medroxyprogesterone Acetate

01 Jan 2019·Molecular and Cellular EndocrinologyQ2 · MEDICINE

Human versus non-human sex steroid use in hormone replacement therapies part 1: Preclinical data

Q2 · MEDICINE

Review

Author: Craig S. Atwood ; Samuel F. Ekstein

Prior to 2002, hormone replacement therapy (HRT) was considered to be an important component of postmenopausal healthcare. This was based on a plethora of basic, epidemiological and clinical studies demonstrating the health benefits of supplementation with human sex steroids. However, adverse findings from the Women's Health Initiative (WHI) studies that examined the 2 major forms of HRT in use in the US at that time - Premarin (conjugated equine estrogens; CEE) and Prempro (CEE + medroxyprogesterone acetate; MPA), cast a shadow over the use of any form of HRT. Here we review the biochemical and physiological differences between the non-human WHI study hormones - CEE and MPA, and their respective human counterparts 17β-estradiol (E₂) and progesterone (P₄). Preclinical data from the last 30 years demonstrate clear differences between human and non-human sex steroids on numerous molecular, physiological and functional parameters in brain, heart and reproductive tissue. In contrast to CEE supplementation, which is not always detrimental although certainly not as optimal as E₂ supplementation, MPA is clearly not equivalent to P₄, having detrimental effects on cognitive, cardiac and reproductive function. Moreover, unlike P₄, MPA is clearly antagonistic of the positive effects of E₂ and CEE on tissue function. These data indicate that minor chemical changes to human sex steroids result in physiologically distinct actions that are not optimal for tissue health and functioning.

27 Nov 2009·BMJ

Pfizer ordered to pay $103m over hormone drugs and breast cancer

Author: Tanne, J. H.

Pfizer, the world’s largest drug company, was ordered to pay $103m (£62m; €68m) in punitive damages to two women this week. The women said they had developed breast cancer after using hormone drugs made by Wyeth and Pharmacia & Upjohn, which are now Pfizer subsidiaries. Pfizer spokesman Chris Loder sent the BMJ the company’s statement saying that it will challenge the verdicts against it. In November a Philadelphia jury decided that the oestrogen-progestogen drug Prempro, sold by Wyeth, caused breast cancer in Connie Barton of Peoria, Illinois, and awarded her $3.7m. Her case is …

01 Apr 2008·The BreastQ2 · MEDICINE

Roles of hormone replacement therapy and iron in proliferation of breast epithelial cells with different estrogen and progesterone receptor status

Q2 · MEDICINE

ArticleOA

Author: Güenther Bernhardt ; Jinlong Jian ; Xi Huang ; Krystyna Frenkel ; Jisen Dai ; Maarten Bosland

Estrogen and iron play critical roles in a female body development and were investigated in the present study in relation to in vitro cell proliferation. Prempro, a hormone replacement therapy drug, and 17beta-estradiol (E2) were shown to increase cell proliferations in estrogen receptor positive (ER+) cells independent of progesterone receptor (PR) status. For example, increased cell proliferation was observed in ER+/PR+ human breast cancer MCF-7, its matching non-cancerous human breast epithelial MCF-12A, and ER+/PR+ murine mammary cancer MXT+ cells, but not in ER-/PR- MDA-MB-231, its matching non-cancerous MCF-10A, and MXT- (ER-/PR+) cells. By mimicking post-menopausal conditions of high estrogen in local breast tissue and increased iron levels due to cessation of menstrual periods, E2 and iron were shown to exert synergistic effects on proliferation of MCF-7 cells and significantly increased Ki67 and proliferating cell nuclear antigen. Western blotting of E2-treated ER+ but not ER- cells showed that E2 also increased transferrin receptor (TfR). Further studies are needed to assess the mitogenic effects of iron and estrogen in normal post-menopausal breast.

100 Deals associated with Conjugated Estrogens/Medroxyprogesterone Acetate

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Conjugated Estrogens/Medroxyprogesterone Acetate	G03AA17 G03AA08	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Osteoporosis, Postmenopausal	US	Wyeth Pharmaceuticals LLC	17 Nov 1995
Vasomotor symptom	US	Wyeth Pharmaceuticals LLC	17 Nov 1995
Vulvovaginal atrophy	US	Wyeth Pharmaceuticals LLC	17 Nov 1995