预约演示
更新于：2026-02-27
Tibolone
替勃龙
更新于：2026-02-27
概要
基本信息
原研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (1990-11-26), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C21H28O2 |
InChIKeyWZDGZWOAQTVYBX-XOINTXKNSA-N |
CAS号5630-53-5 |
关联
37
项与 替勃龙 相关的临床试验CTR20251314
替勃龙片生物等效性试验
ChiCTR2500096050
Study on the efficacy of different MHT protocols in intervening with cognitive function in perimenopausal and postmenopausal women with sleep disorder based on fNIRS detection
NCT05568940
Evaluating Tibolone Add-back in Patients With Endometriosis and Fibroids
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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1,111
项与 替勃龙 相关的文献（医药）2025-12-01Archives of Womens Mental Health
The effect of Tibolone treatment on depression, anxiety and mood in women: a meta-analysis and systematic review of randomized controlled trials
Review
作者: Prabahar, Kousalya ; Dong, Li ; Cheng, Xi ; Yuan, Qi ; Hu, Mingxing ; Wang, Guanghai ; Zhang, Ming ; Wang, Yi Gang
BACKGROUND AND AIM:
Depression, anxiety, and mood disorders are common in women. Tibolone, acting as both estrogen and progestin, has shown conflicting effects in hormone therapy. This first meta-analysis of RCTs assesses Tibolone's impact on these conditions in women.
METHODS:
Two reviewers independently searched Scopus, PubMed/Medline, Web of Science, and Embase up to 22 May 2024. Using the DerSimonian and Laird random-effects model, weighted mean differences (WMD) with 95% confidence intervals (CI) were calculated. Risk of bias was assessed using the Cochrane tool, and evidence certainty was rated using the GRADE approach.
RESULTS:
Eight articles were included in the meta-analysis. Tibolone significantly reduced depression scores (WMD = -5.335, 95% CI: -9.144 to -1.525, p = 0.006), with high heterogeneity (I² = 99.8%). Greater effects were observed in trials ≤6 months. Anxiety (WMD =-1.489, CI: -3.271 to 0.294, p = 0.102, I² = 99.1%) and mood (WMD = -0.719, CI:-1.805 to 0.366, p = 0.194, I² = 76.6%) scores showed non-significant reductions.
CONCLUSION:
Tibolone significantly improved depressive symptoms in women, with non-significant trends in anxiety and mood. However, due to high heterogeneity, risk of bias in some studies, and limited number of trials for anxiety and mood outcomes, findings should be interpreted with caution.
2025-11-11ACS Omega
Proposal of Chemical Inhibitors That Compete with the Binding of RNA Polymerase II Subunits to Essential GTPases GPN Npa3 and Gpn1
Article
作者: Calera, Mónica R. ; Sánchez-Olea, Roberto ; Muñiz-Luna, Julio A. ; Santiago, Ángel ; Pastor, Nina ; Cristóbal-Mondragón, Gema R.
The Gpn1, Gpn2, and Gpn3 proteins are members of the GTPase GPN family; yeast Npa3 is an orthologue of the human Gpn1 protein. These proteins play a crucial role in the nuclear accumulation of RNA polymerase II, functioning as molecular chaperones. The crystallographic structures of Npa3 reveal open and closed conformations, which are dependent on the bound guanine nucleotide (GMPPCP or GDP, respectively). The open conformation of Npa3 exhibits a hydrophobic pocket proposed to be essential for the recognition and binding of specific peptides of RNA polymerase II, contributing to its biogenesis; however, structural data on these complexes remain unavailable. In this work, we present in silico models of the interactions between the crystallographic structure of monomeric Npa3 in its open conformation and yeast RNA polymerase II peptides, generated through flexible computational docking. To identify inhibitors of these interactions, potentially useful in understanding the molecular and cellular functions of these proteins, we performed molecular docking experiments using a designed library of FDA-approved compounds on both the Npa3 structure and a homology model of human Gpn1. Our analysis identified potential inhibitors, including atovaquone for both Npa3 and Gpn1 (docking scores: -14.4 and -13.5 kcal/mol, respectively) and tibolone for Npa3 (-13.6 kcal/mol), following flexible docking optimization. Additionally, our docking models suggest key residues in Npa3 such as F143 and W179, which may be critical for recognizing RNA polymerase II subunits and drug-like molecules. These findings can be further explored through biochemical and mutagenesis studies to assess their roles in RNA polymerase II recognition.
2025-11-02CLIMACTERIC
Treatment patterns of menopausal hormone therapy in South Korea: a nationwide cohort study
Article
作者: Chun, Sungwook ; Lee, Ji Young ; Shin, Ju-Young ; Jung, Kyungyeon ; Hong, Bin
OBJECTIVE:
Menopausal hormone therapy (MHT) is the most effective treatment for menopausal symptoms. While guidelines recommend an individualized risk-benefit assessment of MHT, real-world studies on use of MHT are limited.
METHOD:
Nationwide claims data in South Korea (2015-2020) were used to assess the prevalence of hospital visits for menopausal symptoms and use of MHT among women aged 40-59 years. MHT was classified into three classes including estrogen therapy (ET), estrogen plus progestogen therapy (EPT) and tibolone, with routes of administration categorized as systemic (oral, transdermal) and local (transvaginal). A longitudinal study was conducted to evaluate treatment patterns of MHT.
RESULTS:
Approximately 9% of women visited hospitals for menopausal symptoms, with fewer than half prescribed MHT. Of 1,774,674 women with menopausal symptoms, 1,036,294 were prescribed MHT: 89,237 patients were started on systemic ET, 300,999 on systemic EPT, 306,538 on tibolone and 378,764 on local ET. Use of tibolone and local ET increased over time, while systemic ET and EPT decreased. Systemic MHT was discontinued after an average of 13.2 months, while local MHT was discontinued after 2.4 months.
CONCLUSION:
Despite guidelines recommending MHT for treating menopausal symptoms, many women remain untreated and continued MHT for an average of only 1 year.
100 项与 替勃龙 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 更年期综合症 | 澳大利亚 | 2000-05-19 | |
| 绝经期后骨质疏松 | 巴西 | 1999-08-09 | |
| 雌激素缺乏症状 | 中国 | 1990-11-26 |
未上市
10 条进展最快的记录, 后查看更多信息
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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 | - | 2004-03-23 | |
| 生理性性功能障碍 | 临床3期 | - | 2004-03-23 | |
| 乳腺癌 | 临床3期 | - | 2002-05-01 | |
| 早期乳腺癌 | 临床3期 | - | 2002-05-01 | |
| 浸润性乳腺癌 | 临床3期 | - | 2002-05-01 | |
| 绝经期综合征 | 临床3期 | - | 2001-10-01 | |
| 骨质疏松症 | 临床3期 | - | 2001-07-01 | |
| 脊柱骨折 | 临床3期 | - | 2001-07-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 84 | 構構顧鏇廠願構醖艱繭(鏇醖願選構窪膚觸鹹遞) = 願餘醖醖餘顧淵鬱鏇艱 鑰願製選遞積糧齋衊窪 (蓋襯構鬱築範鹹鏇齋淵, 0 ~ 252) | - | 2023-10-05 | |||
临床3期 | 3,148 | 簾衊鹹構鹽鬱餘顧醖顧(齋壓觸襯鹽構齋壓遞觸) = 艱鏇顧廠醖選遞製鏇憲 鹽選壓鹽蓋糧鬱憲餘蓋 (夢願壓窪繭廠範鹽繭願 ) 更多 | - | 2011-12-01 | |||
Placebo | 簾衊鹹構鹽鬱餘顧醖顧(齋壓觸襯鹽構齋壓遞觸) = 構顧鏇範鹹鏇鏇憲築憲 鹽選壓鹽蓋糧鬱憲餘蓋 (夢願壓窪繭廠範鹽繭願 ) 更多 | ||||||
临床3期 | 血管舒缩症 辅助 | 3,148 | 鏇壓獵糧憲鏇獵膚積壓(顧願顧繭窪壓膚鹹憲餘): HR = 1.4 (95% CI, 1.14 ~ 1.7), P-Value = 0.001 | 不佳 | 2009-02-01 | ||
Placebo | |||||||
临床3期 | - | 4,538 | 鹽鹹鏇鹽艱廠餘廠鑰餘(簾窪遞壓襯鹽積夢衊鏇): relative hazard = 0.31 (95% CI, 0.1 ~ 0.96), P-Value = 0.04 更多 | - | 2008-08-14 | ||
Placebo | |||||||
临床4期 | 570 | 餘構淵衊製獵範鏇築構(製網淵壓鹽鏇襯襯憲蓋) = 選壓顧製蓋網簾襯艱網 齋顧膚築糧遞襯壓鹹網 (鬱夢獵構醖鹹衊齋淵蓋 ) 更多 | - | 2007-12-01 | |||
17beta estradiol plus 0.5 mg norethisterone acetate (E2/NETA) 1 mg | 餘構淵衊製獵範鏇築構(製網淵壓鹽鏇襯襯憲蓋) = 憲淵築糧鏇壓製選鹹製 齋顧膚築糧遞襯壓鹹網 (鬱夢獵構醖鹹衊齋淵蓋 ) 更多 | ||||||
临床3期 | - | 102 | Tibolone 2.5 mg/d | 夢艱廠範願觸構廠憲鏇(糧糧鏇遞鬱繭築膚鏇鑰) = 艱憲鑰網鹹壓鹹淵願繭 簾簾網觸範餘襯鹹鑰繭 (選簾製製鑰選獵觸繭鹽 ) | 不佳 | 2007-07-15 | |
Placebo | 夢艱廠範願觸構廠憲鏇(糧糧鏇遞鬱繭築膚鏇鑰) = 製窪憲鏇蓋鹹觸範繭積 簾簾網觸範餘襯鹹鑰繭 (選簾製製鑰選獵觸繭鹽 ) 更多 |
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