Tibolone
(Synonyms: 替勃龙) 目录号 : GC41153A tissue-selective steroid with estrogenic and androgenic effects
Cas No.:5630-53-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tibolone is an estrogen-like compound used for the treatment of the symptoms associated with menopausal transition (i.e., climacteric symptoms) and also for the treatment of osteoporosis. Three major metabolites of tibolone are responsible for its tissue selective mechanism of action. Conversion into 3α- and 3β-hydroxy-tibolone results in estrogenic effects in brain, vagina, and bone. The δ4 isomer has progestrogenic and androgenic effects and does not cause estrogenic stimulation in the endometrium. A two-year longitudinal study indicates that low doses (1.25-2.5 mg) of tibolone effectively relieve climacteric symptoms and prevent loss of bone mass in early postmenopausal women.
| Cas No. | 5630-53-5 | SDF | |
| 别名 | 替勃龙 | ||
| Canonical SMILES | O[C@@]1(C#C)CC[C@@]2([H])[C@]([C@]3([H])CC[C@@]21C)([H])[C@H](C)CC4=C3CCC(C4)=O | ||
| 分子式 | C21H28O2 | 分子量 | 312.5 |
| 溶解度 | DMF: 30 mg/ml,DMF:PBS (pH 7.2)(1:3): .25 mg/ml,DMSO: 20 mg/ml,Ethanol: 2 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2 mL | 16 mL | 32 mL |
| 5 mM | 0.64 mL | 3.2 mL | 6.4 mL |
| 10 mM | 0.32 mL | 1.6 mL | 3.2 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Tibolone as Hormonal Therapy and Neuroprotective Agent
Trends Endocrinol Metab 2020 Oct;31(10):742-759.PMID:32507541DOI:10.1016/j.tem.2020.04.007.
Tibolone (TIB), a selective tissue estrogenic activity regulator (STEAR) in clinical use by postmenopausal women, activates hormonal receptors in a tissue-specific manner. Estrogenic activity is present mostly in the brain, vagina, and bone, while the inactive forms predominate in the endometrium and breast. Conflicting literature on TIB's actions has been observed. While it has benefits for vasomotor symptoms, bone demineralization, and sexual health, a higher relative risk of hormone-sensitive cancer has been reported. In the brain, TIB can improve mood and cognition, neuroinflammation, and reactive gliosis. This review aims to discuss the systemic effects of TIB on peri- and post-menopausal women and its role in the brain. We suggest that TIB is a hormonal therapy with promising neuroprotective properties.
Short-term and long-term effects of Tibolone in postmenopausal women
Cochrane Database Syst Rev 2016 Oct 12;10(10):CD008536.PMID:27733017DOI:10.1002/14651858.CD008536.pub3.
Background: Tibolone is a synthetic steroid used for the treatment of menopausal symptoms, on the basis of short-term data suggesting its efficacy. We considered the balance between the benefits and risks of Tibolone. Objectives: To evaluate the effectiveness and safety of Tibolone for treatment of postmenopausal and perimenopausal women. Search methods: In October 2015, we searched the Gynaecology and Fertility Group (CGF) Specialised Register, the Cochrane Central Register of Controlled Trials (CENTRAL), MEDLINE, Embase and PsycINFO (from inception), the Cumulative Index to Nursing and Allied Health Literature (CINAHL) and clinicaltrials.gov. We checked the reference lists in articles retrieved. Selection criteria: We included randomised controlled trials (RCTs) comparing Tibolone versus placebo, oestrogens and/or combined hormone therapy (HT) in postmenopausal and perimenopausal women. Data collection and analysis: We used standard methodological procedures of The Cochrane Collaboration. Primary outcomes were vasomotor symptoms, unscheduled vaginal bleeding and long-term adverse events. We evaluated safety outcomes and bleeding in studies including women either with or without menopausal symptoms. Main results: We included 46 RCTs (19,976 women). Most RCTs evaluated Tibolone for treating menopausal vasomotor symptoms. Some had other objectives, such as assessment of bleeding patterns, endometrial safety, bone health, sexuality and safety in women with a history of breast cancer. Two included women with uterine leiomyoma or lupus erythematosus. Tibolone versus placebo Vasomotor symptomsTibolone was more effective than placebo (standard mean difference (SMD) -0.99, 95% confidence interval (CI) -1.10 to -0.89; seven RCTs; 1657 women; moderate-quality evidence), but removing trials at high risk of attrition bias attenuated this effect (SMD -0.61, 95% CI -0.73 to -0.49; odds ratio (OR) 0.33, 85% CI 0.27 to 0.41). This suggests that if 67% of women taking placebo experience vasomotor symptoms, between 35% and 45% of women taking Tibolone will do so. Unscheduled bleedingTibolone was associated with greater likelihood of bleeding (OR 2.79, 95% CI 2.10 to 3.70; nine RCTs; 7814 women; I2 = 43%; moderate-quality evidence). This suggests that if 18% of women taking placebo experience unscheduled bleeding, between 31% and 44% of women taking Tibolone will do so. Long-term adverse eventsMost of the studies reporting these outcomes provided follow-up of two to three years (range three months to three years). Breast cancerWe found no evidence of differences between groups among women with no history of breast cancer (OR 0.52, 95% CI 0.21 to 1.25; four RCTs; 5500 women; I2= 17%; very low-quality evidence). Among women with a history of breast cancer, Tibolone was associated with increased risk (OR 1.5, 95% CI 1.21 to 1.85; two RCTs; 3165 women; moderate-quality evidence). Cerebrovascular eventsWe found no conclusive evidence of differences between groups in cerebrovascular events (OR 1.74, 95% CI 0.99 to 3.04; four RCTs; 7930 women; I2 = 0%; very low-quality evidence). We obtained most data from a single RCT (n = 4506) of osteoporotic women aged 60 to 85 years, which was stopped prematurely for increased risk of stroke. Other outcomesEvidence on other outcomes was of low or very low quality, with no clear evidence of any differences between the groups. Effect estimates were as follows:• Endometrial cancer: OR 2.04, 95% CI 0.79 to 5.24; nine RCTs; 8504 women; I2 = 0%.• Cardiovascular events: OR 1.38, 95% CI 0.84 to 2.27; four RCTs; 8401 women; I2 = 0%.• Venous thromboembolic events: OR 0.85, 95% CI 0.37 to 1.97; 9176 women; I2 = 0%.• Mortality from any cause: OR 1.06, 95% CI 0.79 to 1.41; four RCTs; 8242 women; I2 = 0%. Tibolone versus combined HT Vasomotor symptomsCombined HT was more effective than Tibolone (SMD 0.17, 95% CI 0.06 to 0.28; OR 1.36, 95% CI 1.11 to 1.66; nine studies; 1336 women; moderate-quality evidence). This result was robust to a sensitivity analysis that excluded trials with high risk of attrition bias, suggesting a slightly greater disadvantage of Tibolone (SMD 0.25, 95% CI 0.09 to 0.41; OR 1.57, 95% CI 1.18 to 2.10). This suggests that if 7% of women taking combined HT experience vasomotor symptoms, between 8% and 14% of women taking Tibolone will do so. Unscheduled bleedingTibolone was associated with a lower rate of bleeding (OR 0.32, 95% CI 0.24 to 0.41; 16 RCTs; 6438 women; I2 = 72%; moderate-quality evidence). This suggests that if 47% of women taking combined HT experience unscheduled bleeding, between 18% and 27% of women taking Tibolone will do so. Long-term adverse eventsMost studies reporting these outcomes provided follow-up of two to three years (range three months to three years). Evidence was of very low quality, with no clear evidence of any differences between the groups. Effect estimates were as follows:• Endometrial cancer: OR 1.47, 95% CI 0.23 to 9.33; five RCTs; 3689 women; I2 = 0%.• Breast cancer: OR 1.69, 95% CI 0.78 to 3.67; five RCTs; 4835 women; I2 = 0%.• Venous thromboembolic events: OR 0.44, 95% CI 0.09 to 2.14; four RCTs; 4529 women; I2 = 0%.• Cardiovascular events: OR 0.63, 95% CI 0.24 to 1.66; two RCTs; 3794 women; I2 = 0%.• Cerebrovascular events: OR 0.76, 95% CI 0.16 to 3.66; four RCTs; 4562 women; I2 = 0%.• Mortality from any cause: only one event reported (two RCTs; 970 women). Authors' conclusions: Moderate-quality evidence suggests that Tibolone is more effective than placebo but less effective than HT in reducing menopausal vasomotor symptoms, and that Tibolone is associated with a higher rate of unscheduled bleeding than placebo but with a lower rate than HT.Compared with placebo, Tibolone increases recurrent breast cancer rates in women with a history of breast cancer, and may increase stroke rates in women over 60 years of age. No evidence indicates that Tibolone increases the risk of other long-term adverse events, or that it differs from HT with respect to long-term safety.Much of the evidence was of low or very low quality. Limitations included high risk of bias and imprecision. Most studies were financed by drug manufacturers or failed to disclose their funding source.
Tibolone: a review
Maturitas 1998 Nov 16;30(3):295-305.PMID:9881330DOI:10.1016/s0378-5122(98)00059-0.
Tibolone appears to be at least as efficacious as other forms of hormonal replacement therapy (HRT) on climacteric symptoms. It does not cause withdrawal bleeding when used in women with at least 1 year of amenorrhea. It is, therefore, not indicated in perimenopause because it may cause irregular bleeding. The androgenic action of Tibolone may have a two-fold benefit: on the one hand, it may help depression and libido more than other forms of HRT, while, on the other hand, it may improve some lipid parameters such as Lp(a), and triglycerides. However, this androgenic action, may also be responsible for the reduction of HDL cholesterol, that may thus reduce the beneficial effect of Tibolone on lipids. It is estimated that only 30% of cardiovascular risk protection of HRT is due to improvement of classical lipids parameters while a great role is played by the direct effect of estrogen on vessels. Tibolone, as well as estrogen, has been shown to induce peripheral vasodilatation and also has a direct effect on vascular reactivity thus increasing peripheral blood flow with no changes in blood pressure or cardiac output. Tibolone seems to exert a similar effect as other forms of HRT on markers of bone metabolism and bone mass, but no data is yet available on fracture prevention.
Does Tibolone treatment have favorable effects on obesity, blood pressure, and inflammation? A meta-analysis of randomized controlled trials
Steroids 2022 Feb;178:108966.PMID:35065995DOI:10.1016/j.steroids.2022.108966.
The clinical effects of Tibolone on cardiometabolic markers are an underlying question in postmenopausal women. We aimed to meta-analyze the effects of Tibolone on anthropometric indicators of obesity, blood pressure (BP), and on C-reactive protein (CRP) levels in postmenopausal women. Two independent reviewers searched Scopus, Web of Science, PubMed/Medline, and Embase up to until 20 April 2021. Weighted mean differences (WMDs) and 95% confidence interval (CI) were calculated through the DerSimonian and Laird random-effect models between the Tibolone and the control groups. Data from 20 eligible included showed that Tibolone treatment increased the body mass index (BMI) by 0.23 kg/m2 (95% CI: 0.017 to 0.45, p = 0.03) but did not significantly increase body weight (WMD: 1.128 kg, 95% CI: -1.76 to 4.02, p = 0.44) or waist circumference (WC) (WMD: 0.64 cm, 95% CI: -3.18 to 4.48, p = 0.74). Also, Tibolone treatment neither changed the systolic BP (WMD: 2.60 mmHg, 95% CI: -2.52 to 7.72, p = 0.31) nor the diastolic BP (WMD: 0.711 mmHg, 95% CI: -2.52 to 3.94, p = 0.66), but increased CRP levels by 0.44 mg/L (95% CI: 0.10 to 0.78, p = 0.01). Tibolone treatment administered in postmenopausal women increased BMI and CRP but did not change body weight, WC, and SBP. Diastolic BP decreased after the Tibolone intervention only in the studies lasting 26 weeks versus ˃26 weeks.
Tibolone and climacteric symptoms
Maturitas 1995 Feb;21(2):127-36.PMID:7752950DOI:10.1016/0378-5122(94)00888-e.
Tibolone (Livial) has advantages over other forms of hormone replacement therapy (HRT); it is easy to use and does not induce withdrawal bleeding in postmenopausal women. The evidence for the effect of Tibolone on climacteric symptoms is reviewed and shows that Tibolone is effective in reducing vasomotor symptoms and vaginal dryness. Tibolone's effect on a range of other symptoms such as headache and insomnia is unclear. There are reports that Tibolone improves mood and libido but much of this research is methodologically flawed. Methodologically sound research is required to investigate Tibolone's effect on mood and libido; such a study is in progress.