结合雌激素/醋酸甲羟孕酮(Conjugated Estrogens/Medroxyprogesterone Acetate) - 药物靶点：ER x PR_在研适应症：绝经期后骨质疏松，血管舒缩症，外阴和阴道萎缩_专利_临床

概要

基本信息

药物类型

小分子化药

别名

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

+ [8]

靶点

ER x PR

作用机制

ERs激动剂(雌激素受体家族激动剂)、PR激动剂(孕激素受体激动剂)

治疗领域

心血管疾病内分泌与代谢疾病皮肤和肌肉骨骼疾病+ [1]

在研适应症

绝经期后骨质疏松血管舒缩症外阴和阴道萎缩

非在研适应症-

原研机构

Wyeth AB

在研机构

Wyeth-Ayerst LaboratoriesWyeth Pharmaceuticals LLC

非在研机构

Wyeth AB

最高研发阶段批准上市

首次获批日期

美国 (1995-11-17),

绝经期后骨质疏松血管舒缩症外阴和阴道萎缩

最高研发阶段(中国)-

特殊审评-

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结构

分子式C22H32O3

InChIKeyFRQMUZJSZHZSGN-HBNHAYAOSA-N

CAS号520-85-4

关联

7

项与结合雌激素/醋酸甲羟孕酮相关的临床试验

NCT00630435 / Completed临床1期

An Open-Label, Single-Dose, Randomized, 4-Period, Crossover, Bioequivalence Study of 3 New Formulations of Premarin® /MPA 0.625 mg/2.5 mg Compared With Reference Formulation of Premarin®/MPA in Healthy Postmenopausal Women

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.

开始日期2008-02-01

申办/合作机构

Wyeth AB

NCT00543634 / Completed临床1期

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).

开始日期2007-10-01

申办/合作机构

Wyeth AB

[+1]

NCT00472927 / Completed临床1期

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).

开始日期2007-05-01

申办/合作机构

Wyeth AB

100 项与结合雌激素/醋酸甲羟孕酮相关的临床结果

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100 项与结合雌激素/醋酸甲羟孕酮相关的转化医学

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100 项与结合雌激素/醋酸甲羟孕酮相关的专利（医药）

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40

项与结合雌激素/醋酸甲羟孕酮相关的文献（医药）

2019-01-01·Molecular and Cellular Endocrinology2区 · 医学

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

2区 · 医学

Review

作者: 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.

2009-11-27·BMJ

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

作者: 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 …

2008-04-01·The Breast2区 · 医学

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

2区 · 医学

ArticleOA

作者: 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 项与结合雌激素/醋酸甲羟孕酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	结合雌激素/醋酸甲羟孕酮	G03AA17 G03AA08	-

研发状态

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适应症	国家/地区	公司	日期
绝经期后骨质疏松	美国	Wyeth Pharmaceuticals LLC	1995-11-17
血管舒缩症	美国	Wyeth Pharmaceuticals LLC	1995-11-17
外阴和阴道萎缩	美国	Wyeth Pharmaceuticals LLC	1995-11-17