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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1,155

项与替勃龙相关的文献（医药）

2025-01-01·Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease

Tibolone treatment after traumatic brain injury exerts a sex-specific and Y chromosome-dependent regulation of methylation and demethylation enzymes and estrogen receptors in the cerebral cortex

Article

作者: Garcia-Segura, Luis M ; Grassi, Daniela ; Bautista-Abad, Alvaro ; Lagunas, Natalia ; Garcia-Segura, Luis M. ; Ganchala, Danny ; Ontiveros, Nebai ; Arevalo, Maria-Angeles ; Pinto-Benito, Daniel

Tibolone, a synthetic steroid used for the treatment of climacteric symptoms, displays sex-specific protective actions in exptl. models of brain diseases.Previous in vitro findings suggest that tibolone reduces oxidative stress and neuroinflammation through the regulation of DNA methylation and the activation of estrogen receptors (ERs) α and β.In this study, we assessed whether tibolone regulates the expression of genes coding for DNA methylation and demethylation enzymes and ERs in the injured cerebral cortex of animals suffering a traumatic brain injury.The four-core genotype mouse model was used to determine whether the effect of tibolone on gene regulation was influenced by gonads or by cell-autonomous actions of sex chromosomes.Tibolone treatment resulted in sex-specific modification in the expression of genes coding for DNA Me transferases (Dnmt) 3a, and 3b, for growth arrest and DNA-damage-inducible proteins (Gadd) 45β and 45γ, and for ERα and ERβ.In contrast, tibolone did not affect the expression of genes coding for Dnmt1, Gadd45α, and ten-eleven translocation methylcytosine dioxygenases 1-3.The sex-specific effect of tibolone on Dnmt3a expression depended on gonadal sex.In contrast, the presence or absence of the Y chromosome determined the effect of tibolone on Dnmt3b, Gadd45β, Gadd45γ, ERα and ERβ expression.These findings suggest that tibolone exerts a sex-specific regulation of DNA methylation and ER expression in the injured cerebral cortex that is determined by a combination of gonadal effects and cell-autonomous actions of sex chromosome genes.

2024-12-01·Maturitas

Menopause and endometriosis

Review

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

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·Biomedical Papers

The renoprotective effect of Tibolone in sepsis-induced acute kidney injury

Article

作者: Erbas, Oytun ; Bora, Ejder Saylav ; Arda, Duygu Burcu

INTRODUCTIONSepsis-induced acute kidney injury (AKI) remains a major challenge in intensive care, contributing significantly to morbidity and mortality. Tibolone, known for its neuroprotective and hormonal properties, has not been explored for its potential in AKI management. This study investigates the protective effects of Tibolone and its underlying mechanisms involving Sirtuin-1 (SIRT1) and Yes-Associated Protein (YAP) in a rat sepsis model.MATERIALS AND METHODSThirty-six female Wistar albino rats underwent cecal ligation and puncture (CLP) to induce sepsis. They were randomly assigned to control, CLP+Saline, and CLP+Tibolone groups. Tibolone was administered intraperitoneally. Biomarkers, including Sirtuin (SIRT1), Yes-associated protein (YAP), Tumor necrosis factor (TNF-α), High mobility group box 1 (HMGB1), malondialdehyde (MDA), creatinine, and urea, were assessed. Histopathological examination evaluated renal damage.RESULTSTibolone administration significantly reduced plasma TNF-α, HMGB1, MDA, creatinine, and urea levels compared to the CLP+Saline group. Moreover, Tibolone elevated SIRT1 and YAP levels in kidney tissues. Histopathological examination demonstrated a significant decrease in tubular epithelial necrosis, luminal debris, dilatation, hemorrhage, and interstitial inflammation in Tibolone-treated rats.CONCLUSIONThis study unveils the protective role of Tibolone against sepsis-induced AKI in rats. The improvements in inflammatory and oxidative biomarkers and histological evidence suggest Tibolone's potential as a therapeutic intervention in sepsis-associated kidney injury. The upregulation of SIRT1 and YAP indicates their involvement in Tibolone's renoprotective mechanisms. Further investigations are warranted to explore Tibolone's translational potential in human sepsis-induced AKI.

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
生理性性功能障碍	临床1期	-	Merck Sharp & Dohme Corp.	2004-03-23
性功能障碍	药物发现	-	Organon & Co.	2004-03-23
乳腺癌	药物发现	-	Merck Sharp & Dohme Corp.	2002-05-01
早期乳腺癌	药物发现	-	Organon & Co.	2002-05-01
绝经期综合征	药物发现	-	Merck Sharp & Dohme Corp.	2001-10-01
骨质疏松症	药物发现	-	Merck Sharp & Dohme Corp.	2001-07-01
绝经期后骨质疏松	药物发现	-	Organon & Co.	2001-07-01
脊柱骨折	药物发现	-	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	選積鬱艱構積網蓋夢襯(鹹壓醖齋獵壓膚衊觸觸) = 憲鏇網構衊齋築鹹衊遞遞獵壓構鏇廠鏇鏇淵憲 (繭簾鑰製齋鏇觸選窪積 ) 更多	-	2011-12-01
				Placebo	選積鬱艱構積網蓋夢襯(鹹壓醖齋獵壓膚衊觸觸) = 膚糧繭廠簾壓觸構願鹹遞獵壓構鏇廠鏇鏇淵憲 (繭簾鑰製齋鏇觸選窪積 ) 更多
NCT00408863 (P05885, Pubmed \| Lancet Oncol)	临床3期	血管舒缩症辅助	3,148	Tibolone 2.5 mg	選鏇廠齋鬱衊廠鬱鹹積(繭獵觸壓遞衊夢窪網繭): 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	蓋鹹鏇壓鏇鑰觸簾廠鬱(願鏇鹽齋蓋鏇艱獵壓襯): 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	糧製淵範艱鏇構醖範積(艱觸積醖壓醖遞憲憲糧) = 築窪願餘築壓夢齋衊選艱繭壓襯餘顧窪醖餘觸 (製構衊淵築衊遞繭襯襯 ) 更多	-	2007-12-01
				17beta estradiol plus 0.5 mg norethisterone acetate (E2/NETA) 1 mg	糧製淵範艱鏇構醖範積(艱觸積醖壓醖遞憲憲糧) = 鏇糧網憲積鏇鏇構憲繭艱繭壓襯餘顧窪醖餘觸 (製構衊淵築衊遞繭襯襯 ) 更多