While there are many medical options for managing endometriosis and fibroids, GnRH-agonist (GnRH-a) therapy remains a very common method of treating these complex conditions. Although this therapy is effective, it does come with significant menopausal side effects, such as hot flashes, sweating, mood changes, sleep disturbance, altered sex drive, decreased bone density, and vaginal and urinary symptoms.
In short, chemically-induced menopause (menopause triggered by GnRH-a injection) causes the same symptoms of natural menopause, but with a sudden onset in a generally young and active population. Low dose hormone add-back therapy is commonly used to lessen these side effects of GnRH-a use.
There are many menopausal hormone therapies (MHTs) used in menopausal women that can help, but few studies have directly evaluated the different options of treatment for women undergoing chemically-induced menopause. Tibolone is a menopausal hormone therapy (MHT) that stands out as a good option in the management of medical menopause in endometriosis patients because it may give fewer side effects than other alternatives and have a positive effect on mood and libido.
This study aims to see how effective Tibolone is as an add-back therapy in women who are hormonally suppressed with a GnRH-a. For this study, we will recruit pre-menopausal women over the age of 18 years old undergoing therapy with the GnRH-a Lupron.

开始日期2024-09-01

申办/合作机构

Centre universitaire de santé McGill

CTR20234154

/ CompletedN/A

中国绝经后健康女性受试者空腹/餐后单次口服替勃龙片和利维爱®的单中心、随机、开放、两序列、四周期、完全重复交叉设计的生物等效性试验

主要目的：以长春金赛药业有限责任公司（简称“长春金赛”）的替勃龙片为受试制剂，以N.V.Organon作为上市许可持有人的替勃龙片（商品名：利维爱®）为参比制剂，比较受试制剂和参比制剂在中国绝经后健康女性受试者体内的药代动力学（PK）行为，验证空腹/餐后单次口服两种制剂的生物等效性。次要目的：评价受试制剂和参比制剂在中国绝经后健康女性受试者中的安全性。

开始日期2024-01-06

申办/合作机构

长春金赛药业有限责任公司

NCT06117969

/ Not yet recruiting临床4期IIT

A Prospective Randomized Controlled Study of the Effects of Different Therapy Regimens on Menopausal Sleep Disorders

Sleeping disorders are one of the most common menopausal symptoms, which seriously affect health and life quality of perimenopausal women. Menopausal hormone therapy is an effective treatment for menopausal symptoms, meanwhile, traditional Chinese medicine is also effective to some extent. This prospective randomized controlled study plan to compare the effects of different therapy regimens, including Tibolone and Xiangshao granules, on menopausal sleep disorders.

开始日期2023-12-30

申办/合作机构

北京协和医院

100 项与替勃龙相关的临床结果

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100 项与替勃龙相关的转化医学

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100 项与替勃龙相关的专利（医药）

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1,556

项与替勃龙相关的文献（医药）

2025-02-01·EUROPEAN JOURNAL OF ENDOCRINOLOGY

Association of menopausal hormone therapy with risk of cardiovascular disease in Korean women

Article

作者: Byun, Young Sup ; Kim, Gwang Sil ; Yuk, Jin-Sung ; Yoon, Sang-Hee ; Kim, Dong-Gil ; Han, Gwan Hee ; Kim, Byung Gyu ; Kim, Myoung-Hwan

Abstract:

Objective:

To evaluate the association between various regimens and combinations of menopausal hormone therapy (MHT) and the risk of cardiovascular disease (CVD) in clinical practice.

Design:

This was a population-based cohort study.

Methods:

This population-based cohort study used data from the Health Insurance Review and Assessment Service. The data of women who reported entering menopause at ≥40 years of age with no history of CVD in the national health examination between 2011 and 2014 were extracted. A total of 134 298 pairs were included in the MHT and non-MHT groups after 1:1 propensity score matching. The participants were followed until December, 31, 2020.

Results:

During a median follow-up of 7.9 (IQR 6.9-8.9) years, the incidences of CVD were 146 per 100 000 person/year and 179 per 100 000 person/year for the non-MHT and MHT groups, respectively. After adjusting for covariates, MHT use was associated with an increased CVD risk (hazard ratio [HR], 1.22 [1.14-1.31]) compared with the non-MHT group; the risk was based on an increased risk of stroke and coronary artery revascularization. Tibolone (HR, 1.38, [1.27-1.50]) was associated with increased CVD, but estrogen alone or combined estrogen/progestogen was not. There was no difference in CVD risk, regardless of the type of estrogen agent used. For combined estrogen/progestogen therapy, dydrogesterone was associated with reduced CVD risk.

Conclusions:

There was an increased risk of CVD in MHT users. By regimen, tibolone use was associated with increased risk of CVD, whereas estrogen either alone or in combination with progestogen was not. There was no difference according to the type of estrogen. The type of progestogen seems to modify the results, since dydrogesterone was associated with reduced CVD risk.

2024-12-01·MATURITAS

Menopause and endometriosis

Review

作者: Martini, Ellis ; Tedeschi, Sara ; Camnasio, Cristina Angela ; Morteo, Vittoria ; Nappi, Rossella E. ; Tiranini, Lara ; Cucinella, Laura ; Cassani, Chiara ; Nappi, Rossella E

The shift in paradigm from the belief that endometriosis exclusively affects women of reproductive age has brought attention to its manifestation in postmenopausal patients. Despite this emerging awareness, there remains a dearth of information in the literature regarding postmenopausal endometriosis, with uncertainties surrounding its prevalence, clinical significance, optimal management strategies, and prognosis. Clinical manifestations of endometriosis in menopausal patients lack specificity, with pain onset possible at any stage of life. The primary approach for symptomatic postmenopausal endometriosis continues to be surgical excision, serving both diagnostic and therapeutic purposes while mitigating the risk of coexisting malignancies. Managing the disease in postmenopausal women presents challenges due to possible contraindications for menopausal hormone therapy and the elevated risk of recurrence and malignant transformation. However, conclusive data regarding the appropriateness of menopausal hormone therapy in women with endometriosis or a history of the disease are lacking. Current recommendations lean towards prioritizing combined menopausal hormone therapy formulations or tibolone over estrogen-only therapies due to their potentially higher malignancy risk. The possible increased risk of osteoporosis and cardiovascular disease in postmenopausal women with endometriosis is likely linked to a history of surgical menopause at an earlier age, but more research is warranted. This narrative review summarizes the available literature and provides insights into the intricate connection between endometriosis and menopause, shedding light on pathogenesis, symptoms, oncologic risk, diagnosis, and treatment.

2024-11-01·MATURITAS

Prior pre-eclampsia does not diminish the vascular protective effect of menopausal hormone therapy

Article

作者: Gissler, Mika ; Joensuu, Johanna M ; Mikkola, Tomi S. ; Mikkola, Tomi S ; Joensuu, Johanna M. ; Venetkoski, Minttu ; Ylikorkala, Olavi ; Savolainen-Peltonen, Hanna

OBJECTIVE:

Women with prior pre-eclampsia are at increased risk of cardiovascular disease (CVD). Menopausal hormone therapy (MHT) may affect this risk. We evaluated the impact of MHT use on cardiovascular risk between women with and without prior pre-eclampsia.

STUDY DESIGN AND MAIN OUTCOME MEASURES:

We assessed the occurrence of any CVD, myocardial infarction (MI) and stroke in MHT users (n = 9700) and non-users (n = 19,914) with prior pre-eclampsia, and likewise in MHT users (n = 27,764) and non-users (n = 58,248) without prior pre-eclampsia over the period 1994-2019. Follow-up started at MHT initiation (mean age 50.4 in pre-eclamptic women and 50.3 in non-pre-eclamptic women) and lasted for a mean of 13.3 years.

RESULTS:

The use of MHT in prior pre-eclamptic women was associated with significant risk reductions for any CVD (HR 0.85, 95 % CI 0.78-0.91), MI (HR 0.66, 95 % CI 0.55-0.78) and stroke events (HR 0.71, 95 % CI 0.63-0.81) in comparison with non-users with prior pre-eclampsia. The risk reductions for cardiovascular deaths were even more pronounced (HR 0.43, 95 % CI 0.31-0.59 for any CVD death; HR 0.49, 95 % CI 0.30-0.80 for MI death; HR 0.25, 95 % CI 0.10-0.64 for stroke death). However, none of these risk reductions differed from those seen in MHT users without prior pre-eclampsia. The risk of any CVD decreased already within five years of MHT use in women with prior pre-eclampsia but not in those without prior pre-eclampsia.

CONCLUSIONS:

The use of MHT is associated with reduced CVD risk in women with prior pre-eclampsia. This is important to clinicians considering the initiation of MHT for recently menopausal women with prior pre-eclampsia.

项与替勃龙相关的新闻（医药）

2024-12-23

·奇点网

BMJ：更年期激素疗法的选择不可随意！超90万女性研究揭示，不同绝经激素疗法对心血管健康的影响有所不同丨临床大发现

*仅供医学专业人士阅读参考总开玩笑说“更年期的女人惹不起”，这句看似幽默的调侃，却道出了无数女性在激素波动中挣扎的真实感受，其中蕴含着她们对生理变化的无奈与心理承受的双重压力。更年期是女性生命中重要的转折点，伴随雌激素水平的下降和促卵泡激素水平的升高，这一阶段的许多女性会经历潮热、盗汗、睡眠障碍、焦虑和记忆力减退等症状。绝经激素疗法（MHT）是当前缓解更年期症状的主要治疗手段之一，其通过补充雌激素，单独或联合孕激素进行治疗。可是，这剂良方同时也可能为这些女性的心血管健康埋下隐患。瑞典乌普萨拉大学的Therese Johansson团队发表的最新研究提醒我们，激素治疗有效，但需谨慎选择。他们通过一项基于超过90万人的大规模队列研究发现，不同绝经激素疗法在心血管健康方面的风险表现差异显著。例如，处于绝经过渡期的女性使用替勃龙与动脉血栓风险提高相关，但与静脉血栓风险无关；口服雌孕激素连续联合或序贯疗法与静脉血栓风险提高61%-100%相关，而经皮单用雌激素疗法与任何心血管疾病风险增加无关。这一研究结果揭示了绝经激素疗法的复杂性，为女性在更年期健康管理中提供重要的科学依据。论文于近日发表在《英国医学杂志》[1]。论文首页截图心血管疾病是全球死亡的主要原因，尤其是在女性绝经后，随着年龄增长，心血管疾病的发生率显著上升。尽管激素治疗被广泛用于缓解更年期症状，如潮热、骨质疏松等，但其与心血管疾病之间的关系一直存在争议。二十多年前的观察性研究曾表明[2-4]，更年期激素治疗可能对心血管健康有保护作用，有助于促进血管生成、扩张血管、减少心脏纤维化等。然而随后的随机对照试验却显示出相反的结果[5-8]，提出激素治疗反而会增加心血管事件的风险，尤其是中风，并得出结论认为激素治疗的风险可能大于益处。这一矛盾被归因于人群差异和方法学偏倚。另外随着新型激素治疗方法的出现，关于不同治疗方式的心血管风险仍需进一步探讨。于是，Therese Johansson团队开展这项基于瑞典全国注册数据的观察性研究，通过模拟目标试验的方法，再次评估绝经激素治疗对心血管疾病风险的影响，研究数据的收集时间范围为2007年-2018年。此次研究设计研究共纳入919614名处于绝经过渡期（50-58岁）的女性，大多数女性在这个年龄开始使用绝经激素疗法。她们入组前两年内未使用过绝经激素疗法，曾患心血管疾病、癌症、子宫切除或双侧卵巢切除等疾病的个体被排除。参与者随机入组七个不同激素疗法的治疗组和一个未绝经激素治疗的对照组。通过为期两年的随访，研究观察了缺血性心脏病、脑梗塞、心肌梗塞和静脉血栓等心血管疾病事件的发生率。 2007-2020年绝经激素疗法使用情况结果显示，相比于对照组，单一口服雌激素与静脉血栓风险增加57%相关。口服雌孕激素连续联合疗法与缺血性心脏病风险增加21%、静脉血栓风险增加61%相关。口服雌孕激素序贯疗法与静脉血栓风险提高100%相关。单一口服雌激素治疗与左炔诺孕酮宫内节育系统结合使用，未显著增加任何心血管疾病风险。比起口服，经皮给药方案带来的风险要低一些。经皮雌孕激素疗法与静脉血栓风险增加46%相关，经皮单用雌激素疗法则与任何心血管疾病风险增加无显著关联。研究者们分析其中机制：口服雌激素通过肝脏首过代谢，影响凝血因子的生成，导致促凝因子增加，从而提高静脉血栓栓塞风险；相比之下，经皮雌激素疗法绕过了肝脏首过代谢，对凝血因子的影响较小，因此静脉血栓风险较低。除了补充天然或合成的雌激素，绝经激素治疗方案还包括替勃龙，这是一种组织选择性雌激素活性调节剂，在体内能够转化为多种代谢物，兼有雌激素、孕激素以及弱雄激素活性。结果显示，相比于对照组，替勃龙治疗与总体心血管疾病风险增加52%、缺血性心脏病风险增加46%相关。令人诧异的是，替勃龙会增加动脉血栓的风险，与脑梗塞风险增加97%、心肌梗塞风险增加94%相关，但却未显著增加静脉血栓风险，其中具体机制需进一步查清。七种绝经激素治疗与心血管疾病事件之间的关联（蓝色：意向治疗分析；黄色：依从治疗分析）总之，这项研究重新评估了绝经激素疗法的心血管健康影响，结果表明，对于处于绝经过渡期的女性，不同激素治疗方式在心血管风险方面存在显著差异。这种异质性反映了激素类型、给药途径和治疗组合在生理作用及安全性上的差异性，进一步强调了临床决策中根据患者具体需求制定个体化治疗方案的重要性。参考文献： [1] Johansson T, Karlsson T, Bliuc D, et al. Contemporary menopausal hormone therapy and risk of cardiovascular disease: Swedish nationwide register based emulated target trial. BMJ. 2024;387:e078784. Published 2024 Nov 27. doi:10.1136/bmj-2023-078784 [2]Grodstein F, Stampfer MJ, Manson JE, et al. Postmenopausal estrogen and progestin use and the risk of cardiovascular disease. N Engl J Med1996;335:453-61. doi:10.1056/NEJM199608153350701 pmid:8672166 [3]Grodstein F, Manson JE, Colditz GA, Willett WC, Speizer FE, Stampfer MJ. A prospective, observational study of postmenopausal hormone therapy and primary prevention of cardiovascular disease. Ann Intern Med2000;133:933-41. doi:10.7326/0003-4819-133-12-200012190-00008 pmid:11119394 [4]Varas-Lorenzo C, García-Rodríguez LA, Perez-Gutthann S, Duque-Oliart A. Hormone replacement therapy and incidence of acute myocardial infarction. A population-based nested case-control study. Circulation2000;101:2572-8. doi:10.1161/01.CIR.101.22.2572 pmid:10840007 [5]Hulley S, Grady D, Bush T, et al. Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in postmenopausal women. Heart and Estrogen/progestin Replacement Study (HERS) Research Group. JAMA1998;280:605-13. doi:10.1001/jama.280.7.605 pmid:9718051 [6]Rossouw JE, Anderson GL, Prentice RL, et al., Writing Group for the Women’s Health Initiative Investigators. Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results From the Women’s Health Initiative randomized controlled trial. JAMA2002;288:321-33. doi:10.1001/jama.288.3.321 pmid:12117397 [7]Manson JE, Hsia J, Johnson KC, et al., Women’s Health Initiative Investigators. Estrogen plus progestin and the risk of coronary heart disease. N Engl J Med2003;349:523-34. doi:10.1056/NEJMoa030808 pmid:12904517 [8]Anderson GL, Limacher M, Assaf AR, et al., Women’s Health Initiative Steering Committee. Effects of conjugated equine estrogen in postmenopausal women with hysterectomy: the Women’s Health Initiative randomized controlled trial. JAMA2004;291:1701-12. doi:10.1001/jama.291.14.1701 pmid:15082697 本文作者 | 张艾迪

2024-12-05

·drugs

Tibolone, Oral Estrogen-Progestin Therapy Linked to Risk for Heart Disease

THURSDAY, Dec. 5, 2024 -- Use of tibolone or oral estrogen-progestin therapy is associated with an increased risk for specific cardiovascular diseases, according to a study published online Nov. 27 in The BMJ . Therese Johansson, from Uppsala University in Sweden, and colleagues examined the effect of contemporary menopausal hormone therapy on the risk for cardiovascular disease according to the route of administration. The nationwide emulated target trial involved 919,614 women aged 50 to 58 years between 2007 and 2020 without hormone therapy use in the previous two years. Women were assigned to one of eight treatment groups. Overall, 77,512 women were initiators of any menopausal hormone therapy and 842,102 women were noninitiators. The researchers found that tibolone was associated with an increased risk for cardiovascular disease compared with noninitiation (hazard ratio, 1.52) in intention-to-treat analyses. The risk for ischemic heart disease was increased for initiators of tibolone or oral estrogen-progestin therapy (hazard ratios, 1.46 and 1.21, respectively). The risk for venous thromboembolism was increased in association with oral continuous estrogen-progestin therapy, sequential therapy, and estrogen-only therapy (hazard ratios, 1.61, 2.00, and 1.57, respectively). In per-protocol analyses, tibolone was associated with a higher risk for cerebral infarction and myocardial infarction (hazard ratios, 1.97 and 1.94, respectively). "We found that starting oral combined continuous therapy or tibolone was associated with an increased risk of cardiovascular disease within the first two years of initiation," the authors write. Abstract/Full Text Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床结果

2024-11-28

·drugs

Some HRT Pills May Pose Special Risk for Blood Clots

THURSDAY, Nov. 28, 2024 -- Certain hormone replacement therapy pills appear to increase the risk of heart disease and serious blood clots in women going through menopause , a new study says. Estrogen/progestin pills increased women’s risk of heart disease by 21% and risk of life-threatening blood clots by 61%, researchers found. Similarly, the synthetic hormone pill tibolone increased risk of heart disease by 46% and nearly doubled the risk of stroke and heart attack, results show. However, tibolone did not increase risk of blood clots, “highlighting the varying effects of different hormones on cardiovascular disease,” wrote the research team led by Therese Johansson , a doctoral student with Uppsala University in Sweden. Tibolone is not approved for use in the U.S., and its use has been decreasing in Sweden, researchers noted. “This drop is encouraging; however, in 2018, approximately 1000 women initiated tibolone, which is estimated to have caused one stroke or … heart disease event,” the researchers wrote. Hormone replacement therapy is used to relieve menopause symptoms such as hot flashes and night sweats. For the study, researchers analyzed data on more than 919,000 healthy women in Sweden who were 50 to 58 years of age between 2007 and 2020. Using monthly prescription records, the women were placed in one of seven different groups depending on the type of hormone replacement therapy they’d been given. An eighth group received no hormone therapy. During a monitoring period of two years, more than 24,000 heart-related health problems were recorded. Women who took oral estrogen/progestin or tibolone had an increased risk of heart disease that translates to about 11 new cases for every 1,000 women who start the treatment for one year, researchers said. They found no increased risk of heart disease for hormone replacement therapies applied through the skin using patches, gels or creams. However, these skin applications did increase the risk of dangerous blood clots, results show. These results show that more research is needed to understand how hormone therapy might affect a menopausal woman’s risk of heart disease, researchers said. Hormones like estrogen taken orally are metabolized in the liver, where many of the body’s blood coagulants are produced, researchers said. This could cause the liver to produce more coagulants, increasing the risk of dangerous blood clots. That also could explain why skin hormone therapy doesn’t increase the risk of clots, because they largely bypass the liver during metabolism, researchers added. The new study appears in The BMJ . Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床结果上市批准

100 项与替勃龙相关的药物交易

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KEGG	Wiki	ATC	Drug Bank
D01639	替勃龙	G03CX01	DB09070

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适应症	国家/地区	公司	日期
绝经期后骨质疏松	阿根廷	-	2006-02-16
更年期综合症	澳大利亚	Organon & Co.	2000-05-19
雌激素缺乏症状	中国	Organon & Co.	1990-11-26
内分泌系统疾病	-	-	1988-01-01

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适应症	最高研发状态	国家/地区	公司	日期
性功能障碍	临床3期	-	Organon & Co.	2004-03-23
生理性性功能障碍	临床3期	-	Merck Sharp & Dohme Corp.	2004-03-23
乳腺癌	临床3期	-	Merck Sharp & Dohme Corp.	2002-05-01
早期乳腺癌	临床3期	-	Organon & Co.	2002-05-01
绝经期综合征	临床3期	-	Merck Sharp & Dohme Corp.	2001-10-01
骨质疏松症	临床3期	-	Merck Sharp & Dohme Corp.	2001-07-01
脊柱骨折	临床3期	-	Organon & Co.	2001-07-01

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT00408863 (P05885 \| LIBERATE, Pubmed \| Maturitas)	临床3期	乳腺癌	3,148	Tibolone 2.5mg	獵築網範繭顧網願齋醖(選艱齋壓簾淵鏇積繭獵) = 願獵繭憲醖鹹構艱窪鑰鹽鏇築繭願糧壓製餘壓 (憲鬱蓋窪齋襯醖繭範窪 ) 更多	-	2011-12-01
				Placebo	獵築網範繭顧網願齋醖(選艱齋壓簾淵鏇積繭獵) = 衊鹹糧壓鑰糧簾夢膚艱鹽鏇築繭願糧壓製餘壓 (憲鬱蓋窪齋襯醖繭範窪 ) 更多
NCT00408863 (P05885, Pubmed \| Lancet Oncol)	临床3期	血管舒缩症辅助	3,148	Tibolone 2.5 mg	鹽範鏇繭夢壓製觸簾壓(齋膚製願範淵鏇鹹鹹網): HR = 1.4 (95% CI, 1.14 ~ 1.7), P-Value = 0.001	不佳	2009-02-01
				Placebo
NCT00519857 (P06468, Pubmed \| N Engl J Med)	临床3期	-	4,538	Tibolone	製膚顧衊獵鑰鹽遞廠膚(鬱構鏇鏇鏇膚鹹憲繭網): relative hazard = 0.31 (95% CI, 0.1 ~ 0.96), P-Value = 0.04 更多	-	2008-08-14
				Placebo
NCT00431093 (Pubmed \| BJOG)	临床4期	出血 \| 外阴和阴道萎缩 \| 血管舒缩症	570	Tibolone 2.5 mg	繭醖糧簾鏇鏇餘範艱簾(鹹糧鹹齋遞餘艱窪鏇構) = 網鏇繭獵網選衊餘顧簾簾醖繭製蓋構艱繭築獵 (獵鏇淵廠齋蓋糧艱範夢 ) 更多	-	2007-12-01
				17beta estradiol plus 0.5 mg norethisterone acetate (E2/NETA) 1 mg	繭醖糧簾鏇鏇餘範艱簾(鹹糧鹹齋遞餘艱窪鏇構) = 願顧夢蓋壓鹽簾壓獵觸簾醖繭製蓋構艱繭築獵 (獵鏇淵廠齋蓋糧艱範夢 ) 更多
NCT00725374 (P06469 \| 32971 \| STEM, Pubmed \| Clin Cancer Res)	临床3期	-	102	Tibolone 2.5 mg/d	製憲艱網醖遞衊膚築積(襯鑰醖製襯廠構選鏇鏇) = 選鏇淵簾獵膚積鬱獵憲醖鏇獵廠遞艱衊獵壓齋 (醖醖廠獵鏇醖齋積製鏇 )	不佳	2007-07-15
				Placebo	製憲艱網醖遞衊膚築積(襯鑰醖製襯廠構選鏇鏇) = 夢衊構鏇遞製鏇襯齋壓醖鏇獵廠遞艱衊獵壓齋 (醖醖廠獵鏇醖齋積製鏇 ) 更多