Tibolone: a steroid with a tissue-specific mode of action

@article{Kloosterboer2001TiboloneAS,
  title={Tibolone: a steroid with a tissue-specific mode of action},
  author={H. Kloosterboer},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2001},
  volume={76},
  pages={231-238}
}
  • H. Kloosterboer
  • Published 2001
  • Medicine, Biology
  • The Journal of Steroid Biochemistry and Molecular Biology
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… Expand
Tissue-selective effects of tibolone on the breast.
TLDR
Clinical studies have shown that tibolone users experience less breast tenderness and do not show an increase in mammographic density as found with continuous combined EPT, and the data concerning tibolin and breast cancer risk are inconclusive and require further investigation. Expand
Progestagenic Effects of Tibolone on Human Endometrial Cancer Cells
TLDR
An endometrial carcinoma cell line (Ishikawa PRAB-36) was used to investigate the progestagenic properties of tibolone and its metabolites and it was found that 3β-OH-tibolon also induces some inhibition of growth. Expand
Tibolone for postmenopausal women: systematic review of randomized trials.
TLDR
The results from the randomized, controlled, and double blind trials of tibolone are discussed, with respect to its effects on climacteric symptoms, sexual function, endometrial and breast tissue, lipid metabolism, and bone mineral density. Expand
In vivo and in vitro estrogenic and progestagenic actions of Tibolone.
TLDR
Transvaginal sonography demonstrated that postmenopausal women treated with Tibolone displayed a thinner endometrium than in the late proliferative phase, but had a phenotype characteristic of the secretory phase, thus demonstrating the estrogenic and progestagenic actions of this SERM. Expand
Pros and cons of existing treatment modalities in osteoporosis: a comparison between tibolone, SERMs and estrogen (±progestogen) treatments
TLDR
It is clear that tibolone is a unique compound with a specific mode of action and that it belongs to a separate class of compounds that can best be described as selective, tissue estrogenic activity regulators (STEARs). Expand
The need for tissue selective menopausal agents
  • J. Eden
  • Medicine
  • Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology
  • 2005
TLDR
One of which (LIBERATE) aims to test the safety of tibolone (vs placebo) in women with a history of breast cancer who are suffering from climacteric symptoms, one of which is key large, placebo-controlled international trials currently underway. Expand
Cardiovascular effects of tibolone: a selective tissue estrogenic activity regulator.
TLDR
The current review focuses on the effects of tibolone on the cardiovascular system and discusses clinical investigations with this compound in postmenopausal women. Expand
CLINICAL REVIEW 140 Tibolone for Postmenopausal Women: Systematic Review of Randomized Trials
TLDR
The results from the randomized, controlled, and double blind trials of tibolone are discussed, with respect to its effects on climacteric symptoms, sexual function, endometrial and breast tissue, lipid metabolism, and bone mineral density (BMD). Expand
Estrogenic effects of 7α-methyl-17α-ethynylestradiol: a newly discovered tibolone metabolite
Abstract Tibolone is a synthetic steroid that is prescribed to postmenopausal women for relief of climacteric symptoms and prevention of osteoporosis. It has been reported to be metabolized in aExpand
Effects of tibolone on the breast of postmenopausal women.
TLDR
It is concluded that tibolone, if not superior to conventional HT, may be more acceptable to clinicians as a therapeutic drug option for use with symptomatic menopausal women. Expand
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Results from this study have confirmed that tibolone and its metabolites can inhibit E1-STS activity and may explain the absence of breast stimulation as observed in clinical studies. Expand
Tibolone: a review.
TLDR
Tibolone appears to be at least as efficacious as other forms of hormonal replacement therapy (HRT) on climacteric symptoms and seems to exert a similar effect as other form of HRT on markers of bone metabolism and bone mass, but no data is yet available on fracture prevention. Expand
Tibolone, a Steroid with a Tissue‐Specific Hormonal Profile, Completely Prevents Ovariectomy‐Induced Bone Loss in Sexually Mature Rats
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Treatment with tibolone for 4 weeks prevented OVX‐induced bone loss by suppressing both bone resorption and bone turnover in a similar way as EE2, however, the frequency of dosing is more important for EE2 than for tIBolone. Expand
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TLDR
The overall effect on hemostatic factors of the present doses of tibolone in healthy, late postmenopausal women tends towards increased fibrinolysis and unchanged coagulation, which may be beneficial and might theoretically counterbalance the potentially negative effect of the decrease in high density lipoprotein cholesterol. Expand
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For the postmenopausal woman, the availability of non-bleeding HRT has great appeal, and compliance is substantially improved, and other clinical situations in which tibolone is particularly useful include: women who has had hormone-dependent tumors in the past, women who have had endometriosis and women taking gonadotropin-releasing hormone agonists. Expand
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Tibolone has the intrinsic potential to be a compound that protects the arterial vessel wall against atherosclerotic processes and counteracted its atheroprotective effect on the vessel wall. Expand
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TLDR
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