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CAS 23454-33-3 Tibolone Acetate / Livial Trenbolone Steroid for Muscle Gainning

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CAS 23454-33-3 Tibolone Acetate / Livial Trenbolone Steroid for Muscle Gainning

Brand Name : Tibolone
Model Number : Tibolone
Certification : GMP/ISO9001
Place of Origin : China
MOQ : 1g
Price : Negotiation
Payment Terms : L/C, Western Union, MoneyGram
Supply Ability : 10000kg/month
Delivery Time : Within 3-7 work days after payment confirmed.
Packaging Details : Customized
Name : Tibolone
CAS : 5630-53-5
MF : C21H28O2
MW : 312.45
EINECS : 227-069-1
Melting point : 169 °C
refractive index : 105 ° (C=0.54, CH2Cl2/Et2O)
storage temp. : 2-8°C
Color : white to beige
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CAS 23454-33-3 Tibolone Acetate / Livial Trenbolone Steroid for Muscle Gainning

Tibolone Description

Tibolone is a synthetic steroid hormone drug, which is fairly non-selective in its binding profile, acting as an agonist mainly at estrogen receptors, with a preference for ER alpha. It is used mainly for treatment of endometriosis,as well as hormone replacement therapy in post-menopausal women. Tibolone has similar or greater efficacy compared to older hormone replacement drugs, but shares a similar side effect profile.It has also been investigated as a possible treatment for female sexual dysfunction.

Tibolone works by mimicking the activity of the female sex hormones, oestrogen and progesterone. It also has some male hormone (androgen) effects. Tibolone helps to restore the balance of female hormones in women who have a lack of oestrogen; it helps to ease symptoms such as hot flushes and night sweats. You will only be prescribed it if these symptoms seriously interfere with your daily life.

Tibolone (Livial/Liviella) is used mainly for treatment of endometriosis, as well as hormone replacement therapy in post-menopausal women. Tibolone is a synthetic steroid hormone drug, which is fairly non-selective in its binding profile, acting as an agonist mainly at estrogen receptors, with a preference for ER alpha. Tibolone has similar or greater efficacy compared to older hormone replacement drugs, but shares a similar side effect profile. It has also been investigated as a possible treatment for female sexual dysfunction.

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In postmenopausal women tibolone has proved to prevent bone-loss and relieve climacteric symptoms as effectively as estrogens, but it does not stimulate the endometrium and the breast. This clinical profile strongly suggests that tibolone is a compound with tissue-specific action. Tibolone is quickly metabolized into its main active metabolites, 3alpha and 3beta-OH, which are also present in an inactive, sulphated, form. In addition a Delta4-metabolite is found in circulation. The 3-OH-metabolites bind only to the estrogen receptor while the Delta4-isomer shows affinity only to the progesterone and androgen receptors. Tibolone prevents bone loss in a similar way to estrogens. Studies on bone mass using anti-estrogen, antiprogestin and anti-androgen in combination with tibolone, confirmed the sole involvement of the estradiol receptor. Increases in skin temperature as well as vaginal atrophy can be prevented by tibolone in a similar way to estrogens. Breast safety studies showed that tibolone clearly inhibited the growth of tumors in a DMBA model. In breast cell lines, tibolone profoundly inhibited sulphatase activity and an increase in apoptosis and decrease in cell proliferation was found. The stimulation of the endometrium is prevented by the local formation of the Delta4-isomer from tibolone or the 3beta-OH-metabolite. We conclude that tibolone acts as a tissue-specific compound by mediating its effects via steroid receptors and enzymatic pathways. This dual effect of tibolone explains it's positive clinical effects on bone, vagina and brain, and avoids stimulation of the endometrium and breast tissue.


In itself Tibolone has no biological activity; the effects are produced mainly by the results of the activity of its metabolites on various tissues. After administration, Tibolone is quickly metabolized into 3¦Á-hydroxytibolone and 3--hydroxytibolone compounds, which are also present in an inactive, sulfated form. A third compound, the ¦¤4- isomer is formed from Tibolone directly or from the 3h hydroxymetabolite.

Tibolone has estrogenic effects on bone and vaginal tissue. The 4-isomer functions as a progestogen in endometrial tissue, whereas in the brain and liver it has androgenic effects.In breast tissue, Tibolone acts by strongly inhibiting sulfate activity and weak inhibition of 17¦Á-hydroxysteroid dehydrogenase activity, which results in blocking the conversion of estrone sulfate to E2.

Tibolone Contraindications;Tibolone is contraindicated in patients with the following conditions:,Women with hormone treated tumors,Undiagnosed vaginal bleeding,Pregnancy/lactation,Liver and/or cardiac disease,Tibolone Adverse Drug Effects,Depression,Diarrhea, constipation, nausea, vomiting or abdominal pain,Visual disturbances,Alteration in results of liver function tests,Excessive fluid retention in the body tissues resulting in swelling (edema),weight changes, vaginal bleeding, pain in the muscles and joints, rashes or itching,Seborrhoeic dermatitis,Headaches, dizziness, growth of facial hair.

1.Tibolone Acetate prevents bone loss and reduces spinal fractures .
One uncontrolled English study has suggested that Tibolone Acetate increases breast cancer risk but better quality placebo controlled randomised trials do not show that breast cancer rates in healthy women are changed by Tibolone Acetate .Tibolone Acetate does not increase breast density .

2.Tibolone Acetate may interfere with the effectiveness of breast cancer therapies and its use is contraindicated in women with breast cancer .

3.Regular mammograms and breast examination are advisable for all women.
Tibolone Acetate decreases total and LDL cholesterol and triglyceride levels. However, it also decreases HDL cholesterol. The impact of these changes are not clear.

4.Recent research suggests that Tibolone Acetate increases the risk of stroke [5]. This risk is mainly seen in women over 60 years of age. The increase among women in their 50s is 4 extra cases per 1000 and among women in their 60s, an extra 13 cases per 1000 women.

5.Tibolone Acetate should not be used for cardiovascular protection.Few data are available with regard to thrombosis risk are available and the outcomes are inconclusive.

6.Although the menopause is a generic physiologic event, its biology is variable and specific to a given individual. Genetically determined distribution and polymorphism of relevant hormone receptors, enzymes, and various cofactors are the biologic mechanisms controlling an individual's clinical response to endogenous and prescribed hormones.

7.Advances in molecular biology have led to the development of newer pharmacologic agents that are tailored to meet specific therapeutic objectives, based on the hormonal biology of relevant organs. Tibolone Acetate, an analogue of the progestin, norethynodrel, is a drug with tissue-specific effects on receptors and enzymes that influences the synthesis and metabolism of endogenous estrogen, progesterone, and androgen. This is achieved via the intestinal bioconversion of Tibolone Acetate into metabolites that have tissue-specific agonistic and/or antagonistic estrogenic (3alpha and 3beta hydroxyTibolone Acetate) and progestogenic/androgenic (delta4 Tibolone Acetate) properties.

8.The postmenopausal synthesis and metabolism of estrogen and androgen are briefly reviewed with particular reference to sex steroid activity in various target organs. On the basis of this hormonal physiology, the clinical utility of Tibolone Acetate is reviewed as a therapeutic agent for the treatment of the symptomatic menopause. The effects of Tibolone Acetate on bone health and osteoporosis, cardiovascular disease, the breast, and the endometrium are summarized, and its role in clinical practice is reviewed.

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