戊酸雌二醇/醋酸甲羟孕酮(Estradiol Valerate/Medroxyprogesterone Acetate) - 药物靶点：ER x PR_在研适应症：更年期综合症，绝经期后骨质疏松_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Estradiol valerate/Medroxyprogesterone、Divina、Divina Nova

+ [5]

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

内分泌与代谢疾病皮肤和肌肉骨骼疾病其他疾病

在研适应症

更年期综合症绝经期后骨质疏松

非在研适应症-

原研机构

Orion Oyj

在研机构

Orion Oyj

非在研机构-

最高研发阶段批准上市

首次获批日期

法国 (1984-01-01),

更年期综合症绝经期后骨质疏松

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

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关联

2

项与戊酸雌二醇/醋酸甲羟孕酮相关的临床试验

NCT05280028 / RecruitingN/AIIT

The Impact of Different Hormone Therapy Regimens on Overactive Bladder Symptoms, Sexual Function, Depressive Symptoms, Autonomic Function, and Arterial Stiffness

Therefore, the aim of this study is to assess the therapeutic effect on overactive bladder symptoms, sexual function, heart rate variability, arterial stiffness, atherosclerosis, sleep, and depression between tibolone and E2V/MPA.
From the results, the investigators will compare the effect of tibolone versus E2V/MPA on overactive bladder symptoms, sexual function, autonomic function, arterial stiffness, atherosclerosis, sleep and depression.

开始日期2022-02-07

申办/合作机构

医疗财团法人徐元智先生医药基金会亚东纪念医院

NCT00294463 / Completed临床4期IIT

Effects of Tibolone Treatment on the Endometrium

Tibolone, a tissue-selective compound with a combination of estrogenic, progestogenic and androgenic properties, is used as an alternative for estrogen or estrogen plus progesterone hormone therapy for the treatment of symptoms associated with menopause and osteoporosis. The current study compares endometrial histology, biochemistry (hormone levels) and gene-expression profiles after short-term (21-days) treatment with tibolone, to the findings after treatment with estradiol-only (E2) and E2+Medroxyprogesterone Acetate (MPA) in healthy postmenopausal women undergoing hysterectomy for endometrial prolaps.
Since short-term tibolone use results in increased spotting and bleeding but long-term treatment with tibolone has been shown to lead to an atrophic endometrium our hypothesis is that tibolone first displays a more estrogenic mode of action, which over time, is counterbalanced by tibolone's progestagenic properties

开始日期2003-02-01

申办/合作机构

Erasmus MC

[+1]

100 项与戊酸雌二醇/醋酸甲羟孕酮相关的临床结果

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100 项与戊酸雌二醇/醋酸甲羟孕酮相关的转化医学

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100 项与戊酸雌二醇/醋酸甲羟孕酮相关的专利（医药）

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8

项与戊酸雌二醇/醋酸甲羟孕酮相关的文献（医药）

2008-06-01·Menopause International

A 10-year follow-up of the effect of continuous-combined hormone replacement therapy and its discontinuation on bone in postmenopausal women

Article

作者: Timonen, Ulla ; Heikkinen, Jorma ; Haapalahti, Jouko ; Vaheri, Raija

Objective To establish the effect on bone mineral density (BMD) of long-term (nine years) continuous-combined hormone replacement therapy (ccHRT) with estradiol valerate/medroxyprogesterone acetate (E2V/MPA) and follow-up one year after discontinuation of ccHRT. Study design A total of 279 women were treated with daily dosages of E2V + MPA: 1 mg + 2.5 mg (n = 69), 1 mg + 5 mg (n = 70) or 2 mg + 5 mg (n = 140) (Indivina®, Orion Pharma, Espoo, Finland) for 8.5 years; all subjects received the lowest dosage for the next six months. BMD was measured at baseline, between 6 and 12 months, annually until the end of study and at one-year postdiscontinuation of ccHRT. Main outcome measure Change in BMD during nine years of treatment with ccHRT and at one-year post-discontinuation of ccHRT. Results Progressive increase of vertebral BMD was observed with all dosage regimens throughout nine years, with corresponding reduction in the proportion of women fulfilling criteria for osteoporosis or osteopaenia. Femoral neck BMD reached a peak at about five to six years, whereas in the lumbar spine the BMD increase was sustained until the end of the study treatment. Mean BMD declined after cessation of ccHRT use but remained substantially above baseline levels. In a subset of women (n = 58) there was a rapid (≤4%) loss of vertebral BMD in the year after termination of ccHRT use. These women had lower than average BMD at baseline but no other factor was identified that distinguished them from the overall study population. Conclusions Low-dose ccHRT in postmenopausal women is associated with increases in lumbar spine BMD for at least nine years. These gains are not sustained after cessation of therapy but the rate of BMD loss varies between individuals.

2005-12-01·British Menopause Society Journal

Decade-long use of continuous combined hormone replacement therapy is associated with better health-related quality of life in postmenopausal women, as measured by the generic 15D instrument

Article

作者: Heikkinen, Jorma ; Ylikangas, Stiina ; Sintonen, Harri

Objective: To examine quality of life after a decade of continuous combined hormone replacement therapy. Study design: The 15D, a generic health-related quality-of-life (HRQoL) instrument, was used to evaluate trends in HRQoL in women who used continuous combined hormone replacement therapy (ccHRT; Indivina®, Orion Pharma, Finland) for up to nine years. These women had a mean age of 56 years of age at the start of therapy. Control data on HRQoL were obtained from age-matched women participating in Finnish population health surveys. Results: Relative to controls, ccHRT was associated with significantly better HRQoL after six and nine years of treatment. Dose minimization at 8.5 years was not associated with a decline in HRQoL in the ensuing six months. One year after discontinuation of ccHRT there was evidence of a decline in HRQoL in women who discontinued ccHRT as planned, whereas HRQoL was maintained in women who had continued or resumed ccHRT during the one-year post-study follow-up. The benefits of ccHRT were apparent in multiple dimensions of the 15D, being largest and most robustly reproduced in the dimension 'discomfort and symptoms'. It is conjectured that the effectiveness of ccHRT in relieving symptoms of menopause may have contributed to the improved HRQoL scores registered in other dimensions, in addition to any direct effects of ccHRT on specific aspects of those other dimensions. Conclusions: These data indicate that up to 10 years of low-dose ccHRT has sustained value in the enhancement of HRQoL when used by women for whom relief of symptoms of menopause and control of bleeding are primary objectives of treatment.

2004-01-01·Climacteric4区 · 医学

Endometrial safety and tolerability of triphasic sequential hormone replacement estradiol valerate/medroxyprogesterone acetate therapy regimen

4区 · 医学

Article

作者: study groups ; H. Kuhl ; L. Mattila ; M. Engelstein ; M. Mustonen ; M. C. P. Rees ; J. Mäenpää

OBJECTIVETwo randomized comparative multicenter studies were conducted to establish the endometrial safety and tolerability of a triphasic sequential hormone replacement estradiol valerate/medroxyprogesterone acetate (E2V/MPA) therapy regimen.METHODSStudy 1 was a randomized, double-blind, clinical phase III study in 399 postmenopausal women, following parallel-group design with two groups. The duration of study treatment was 12 or 13 cycles of 28 days. A double-dummy technique was used to ensure blinding in the study. The investigational drugs were E2V/MPA triphasic and E2V/MPA biphasic (Diviseq and Divina, respectively; Orion Pharma). In study 2, a total of 341 subjects were randomly allocated by computer into two parallel groups receiving either E2V/MPA or estradiol/norethisterone acetate triphasic (E2/NETA, Trisequens; Novo Nordisk A/S) for 12-13 cycles. The study was an open, clinical phase III trial with a randomized, parallel-group design. Endometrial biopsies combined with transvaginal ultrasound were undertaken before and at the end of treatment during the progestogen phase. Bleeding patterns and symptom control were assessed throughout both studies.RESULTSE2V/MPA triphasic was found to have similar endometrial effects and bleeding patterns to those with E2V/MPA biphasic and E2/NETA triphasic. Climacteric symptoms were relieved as quickly and effectively as with the two comparator treatments. No adverse drug reactions specific to E2V/MPA triphasic were observed. At the end of the study, the proportions of secretory samples were 67.1% for the combined E2V/MPA triphasic groups, 65.6% for the E2V/MPA biphasic group and 71.6% for the E2/NETA triphasic group. One case of hyperplasia occurred in the E2V/MPA triphasic group. Thus the incidence of hyperplasia for the combined groups was 0.33%.CONCLUSIONSThe triphasic E2V/MPA regimen was well tolerated and produced endometrial effects similar to those of the two comparators. Extending estrogen during the so-called treatment-free week with a lower dose of estradiol was effective in controlling vasomotor symptoms.

100 项与戊酸雌二醇/醋酸甲羟孕酮相关的药物交易

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